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Gefitinib
Synonyms: ZD1839
Gefitinib is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.
Gefitinib Chemical Structure
CAS: 184475-35-2
Selleck's Gefitinib has been cited by 707 publications
Purity & Quality Control
Batch:
Purity:
99.98%
99.98
Other EGFR Products
Related compound libraries
Choose Selective EGFR Inhibitors
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| NCI-H1975 | Growth Inhibition Assay | IC50=21.461 μM | SANGER | |||
| HT | Growth Inhibition Assay | IC50=21.4331 μM | SANGER | |||
| HUTU-80 | Growth Inhibition Assay | IC50=21.4336 μM | SANGER | |||
| PA-1 | Growth Inhibition Assay | IC50=21.2787 μM | SANGER | |||
| HOP-62 | Growth Inhibition Assay | IC50=21.2784 μM | SANGER | |||
| GI-1 | Growth Inhibition Assay | IC50=21.17 μM | SANGER | |||
| MC116 | Growth Inhibition Assay | IC50=21.0723 μM | SANGER | |||
| A375 | Growth Inhibition Assay | IC50=21.0567 μM | SANGER | |||
| IST-SL1 | Growth Inhibition Assay | IC50=20.7879 μM | SANGER | |||
| TE-5 | Growth Inhibition Assay | IC50=20.7482 μM | SANGER | |||
| SiHa | Growth Inhibition Assay | IC50=20.3712 μM | SANGER | |||
| LB2518-MEL | Growth Inhibition Assay | IC50=20.3739 μM | SANGER | |||
| BB49-HNC | Growth Inhibition Assay | IC50=19.92 μM | SANGER | |||
| HGC-27 | Growth Inhibition Assay | IC50=20.1394 μM | SANGER | |||
| Becker | Growth Inhibition Assay | IC50=19.8547 μM | SANGER | |||
| TYK-nu | Growth Inhibition Assay | IC50=19.8378 μM | SANGER | |||
| NCI-H650 | Growth Inhibition Assay | IC50=19.7508 μM | SANGER | |||
| WM-115 | Growth Inhibition Assay | IC50=19.6774 μM | SANGER | |||
| HuH-7 | Growth Inhibition Assay | IC50=19.7421 μM | SANGER | |||
| NCI-N87 | Growth Inhibition Assay | IC50=19.5992 μM | SANGER | |||
| NCI-H1048 | Growth Inhibition Assay | IC50=19.2326 μM | SANGER | |||
| NCI-H446 | Growth Inhibition Assay | IC50=19.3589 μM | SANGER | |||
| NCI-H1437 | Growth Inhibition Assay | IC50=19.0467 μM | SANGER | |||
| D-263MG | Growth Inhibition Assay | IC50=19.0172 μM | SANGER | |||
| MFH-ino | Growth Inhibition Assay | IC50=18.9669 μM | SANGER | |||
| U-266 | Growth Inhibition Assay | IC50=18.8649 μM | SANGER | |||
| OVCAR-8 | Growth Inhibition Assay | IC50=18.9276 μM | SANGER | |||
| KNS-42 | Growth Inhibition Assay | IC50=18.8015 μM | SANGER | |||
| U251 | Growth Inhibition Assay | IC50=18.7347 μM | SANGER | |||
| MFE-280 | Growth Inhibition Assay | IC50=18.7293 μM | SANGER | |||
| NCI-H1563 | Growth Inhibition Assay | IC50=18.7124 μM | SANGER | |||
| MDA-MB-361 | Growth Inhibition Assay | IC50=18.5588 μM | SANGER | |||
| HLE | Growth Inhibition Assay | IC50=18.3148 μM | SANGER | |||
| SW982 | Growth Inhibition Assay | IC50=18.4075 μM | SANGER | |||
| KM-H2 | Growth Inhibition Assay | IC50=17.9411 μM | SANGER | |||
| D-502MG | Growth Inhibition Assay | IC50=17.9808 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=17.8593 μM | SANGER | |||
| SF268 | Growth Inhibition Assay | IC50=17.6969 μM | SANGER | |||
| Calu-6 | Growth Inhibition Assay | IC50=17.6782 μM | SANGER | |||
| SW1783 | Growth Inhibition Assay | IC50=17.6415 μM | SANGER | |||
| NCI-H747 | Growth Inhibition Assay | IC50=17.5297 μM | SANGER | |||
| NCI-H1573 | Growth Inhibition Assay | IC50=17.2826 μM | SANGER | |||
| NCI-H1581 | Growth Inhibition Assay | IC50=17.4411 μM | SANGER | |||
| RKO | Growth Inhibition Assay | IC50=17.0748 μM | SANGER | |||
| MZ2-MEL | Growth Inhibition Assay | IC50=17.133 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=16.9032 μM | SANGER | |||
| LB373-MEL-D | Growth Inhibition Assay | IC50=16.7232 μM | SANGER | |||
| MEL-HO | Growth Inhibition Assay | IC50=16.8854 μM | SANGER | |||
| BEN | Growth Inhibition Assay | IC50=16.5155 μM | SANGER | |||
| M059J | Growth Inhibition Assay | IC50=16.284 μM | SANGER | |||
| D-283MED | Growth Inhibition Assay | IC50=16.4209 μM | SANGER | |||
| GP5d | Growth Inhibition Assay | IC50=16.2187 μM | SANGER | |||
| BHT-101 | Growth Inhibition Assay | IC50=16.2439 μM | SANGER | |||
| HT55 | Growth Inhibition Assay | IC50=15.9478 μM | SANGER | |||
| no-11 | Growth Inhibition Assay | IC50=15.9663 μM | SANGER | |||
| MPP-89 | Growth Inhibition Assay | IC50=15.9417 μM | SANGER | |||
| HuCCT1 | Growth Inhibition Assay | IC50=15.874 μM | SANGER | |||
| NCI-H23 | Growth Inhibition Assay | IC50=15.8438 μM | SANGER | |||
| UMC-11 | Growth Inhibition Assay | IC50=15.7523 μM | SANGER | |||
| MCF7 | Growth Inhibition Assay | IC50=15.8145 μM | SANGER | |||
| COLO-320-HSR | Growth Inhibition Assay | IC50=15.5307 μM | SANGER | |||
| CW-2 | Growth Inhibition Assay | IC50=15.1421 μM | SANGER | |||
| MOLT-4 | Growth Inhibition Assay | IC50=15.0497 μM | SANGER | |||
| NCI-H1755 | Growth Inhibition Assay | IC50=14.9953 μM | SANGER | |||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=14.969 μM | SANGER | |||
| TGBC1TKB | Growth Inhibition Assay | IC50=14.6615 μM | SANGER | |||
| NCI-H630 | Growth Inhibition Assay | IC50=14.9467 μM | SANGER | |||
| LAN-6 | Growth Inhibition Assay | IC50=14.253 μM | SANGER | |||
| A549 | Growth Inhibition Assay | IC50=14.4712 μM | SANGER | |||
| RD | Growth Inhibition Assay | IC50=14.4813 μM | SANGER | |||
| KALS-1 | Growth Inhibition Assay | IC50=13.8525 μM | SANGER | |||
| LOXIMVI | Growth Inhibition Assay | IC50=13.6151 μM | SANGER | |||
| SK-PN-DW | Growth Inhibition Assay | IC50=13.8427 μM | SANGER | |||
| SN12C | Growth Inhibition Assay | IC50=13.3808 μM | SANGER | |||
| NCI-H1993 | Growth Inhibition Assay | IC50=13.4285 μM | SANGER | |||
| G-361 | Growth Inhibition Assay | IC50=12.9129 μM | SANGER | |||
| RH-18 | Growth Inhibition Assay | IC50=13.2962 μM | SANGER | |||
| GT3TKB | Growth Inhibition Assay | IC50=12.6327 μM | SANGER | |||
| DMS-273 | Growth Inhibition Assay | IC50=12.8633 μM | SANGER | |||
| C3A | Growth Inhibition Assay | IC50=12.5785 μM | SANGER | |||
| Daoy | Growth Inhibition Assay | IC50=12.4542 μM | SANGER | |||
| ABC-1 | Growth Inhibition Assay | IC50=12.341 μM | SANGER | |||
| KS-1 | Growth Inhibition Assay | IC50=12.2832 μM | SANGER | |||
| JAR | Growth Inhibition Assay | IC50=12.3369 μM | SANGER | |||
| CAMA-1 | Growth Inhibition Assay | IC50=12.1633 μM | SANGER | |||
| U-118-MG | Growth Inhibition Assay | IC50=12.2441 μM | SANGER | |||
| OE19 | Growth Inhibition Assay | IC50=11.9367 μM | SANGER | |||
| Mo-T | Growth Inhibition Assay | IC50=11.9541 μM | SANGER | |||
| SCC-9 | Growth Inhibition Assay | IC50=11.8151 μM | SANGER | |||
| HOS | Growth Inhibition Assay | IC50=11.8683 μM | SANGER | |||
| UM-UC-3 | Growth Inhibition Assay | IC50=11.7421 μM | SANGER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=11.7252 μM | SANGER | |||
| MLMA | Growth Inhibition Assay | IC50=11.6997 μM | SANGER | |||
| RPMI-7951 | Growth Inhibition Assay | IC50=11.6348 μM | SANGER | |||
| NCI-H1299 | Growth Inhibition Assay | IC50=11.6647 μM | SANGER | |||
| LS-411N | Growth Inhibition Assay | IC50=11.6101 μM | SANGER | |||
| HCC1954 | Growth Inhibition Assay | IC50=11.436 μM | SANGER | |||
| GOTO | Growth Inhibition Assay | IC50=11.5206 μM | SANGER | |||
| FTC-133 | Growth Inhibition Assay | IC50=11.3081 μM | SANGER | |||
| LB831-BLC | Growth Inhibition Assay | IC50=11.2556 μM | SANGER | |||
| HCC38 | Growth Inhibition Assay | IC50=10.9716 μM | SANGER | |||
| SF-295 | Growth Inhibition Assay | IC50=10.9902 μM | SANGER | |||
| K-562 | Growth Inhibition Assay | IC50=10.8395 μM | SANGER | |||
| SW900 | Growth Inhibition Assay | IC50=10.8228 μM | SANGER | |||
| D-336MG | Growth Inhibition Assay | IC50=10.7005 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=10.7967 μM | SANGER | |||
| SW962 | Growth Inhibition Assay | IC50=10.6204 μM | SANGER | |||
| VMRC-RCZ | Growth Inhibition Assay | IC50=10.6749 μM | SANGER | |||
| HEC-1 | Growth Inhibition Assay | IC50=10.4081 μM | SANGER | |||
| A2058 | Growth Inhibition Assay | IC50=10.5491 μM | SANGER | |||
| K5 | Growth Inhibition Assay | IC50=10.3395 μM | SANGER | |||
| U031 | Growth Inhibition Assay | IC50=10.2686 μM | SANGER | |||
| YH-13 | Growth Inhibition Assay | IC50=10.3057 μM | SANGER | |||
| SK-UT-1 | Growth Inhibition Assay | IC50=10.2574 μM | SANGER | |||
| NCI-H810 | Growth Inhibition Assay | IC50=10.1597 μM | SANGER | |||
| DJM-1 | Growth Inhibition Assay | IC50=10.1732 μM | SANGER | |||
| CAL-51 | Growth Inhibition Assay | IC50=10.0877 μM | SANGER | |||
| HCE-4 | Growth Inhibition Assay | IC50=10.1122 μM | SANGER | |||
| NCI-H2342 | Growth Inhibition Assay | IC50=10.0155 μM | SANGER | |||
| A204 | Growth Inhibition Assay | IC50=10.0466 μM | SANGER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=9.94088 μM | SANGER | |||
| SW837 | Growth Inhibition Assay | IC50=9.8482 μM | SANGER | |||
| OCI-AML2 | Growth Inhibition Assay | IC50=9.8696 μM | SANGER | |||
| EFO-21 | Growth Inhibition Assay | IC50=9.58735 μM | SANGER | |||
| C32 | Growth Inhibition Assay | IC50=9.6334 μM | SANGER | |||
| KP-4 | Growth Inhibition Assay | IC50=9.48838 μM | SANGER | |||
| A101D | Growth Inhibition Assay | IC50=9.51719 μM | SANGER | |||
| IA-LM | Growth Inhibition Assay | IC50=9.41966 μM | SANGER | |||
| HPAF-II | Growth Inhibition Assay | IC50=9.22518 μM | SANGER | |||
| Capan-2 | Growth Inhibition Assay | IC50=9.40109 μM | SANGER | |||
| BFTC-909 | Growth Inhibition Assay | IC50=9.18297 μM | SANGER | |||
| RPMI-8226 | Growth Inhibition Assay | IC50=9.11304 μM | SANGER | |||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=9.10579 μM | SANGER | |||
| NCI-H2228 | Growth Inhibition Assay | IC50=9.11081 μM | SANGER | |||
| NCI-H226 | Growth Inhibition Assay | IC50=9.09 μM | SANGER | |||
| D-566MG | Growth Inhibition Assay | IC50=9.0181 μM | SANGER | |||
| LS-1034 | Growth Inhibition Assay | IC50=8.94652 μM | SANGER | |||
| NCI-H1792 | Growth Inhibition Assay | IC50=8.88903 μM | SANGER | |||
| COLO-792 | Growth Inhibition Assay | IC50=8.74946 μM | SANGER | |||
| A673 | Growth Inhibition Assay | IC50=8.67611 μM | SANGER | |||
| D-392MG | Growth Inhibition Assay | IC50=8.66214 μM | SANGER | |||
| EGI-1 | Growth Inhibition Assay | IC50=8.60088 μM | SANGER | |||
| TGBC11TKB | Growth Inhibition Assay | IC50=8.46164 μM | SANGER | |||
| 5637 | Growth Inhibition Assay | IC50=8.31055 μM | SANGER | |||
| KYSE-70 | Growth Inhibition Assay | IC50=8.19761 μM | SANGER | |||
| VM-CUB-1 | Growth Inhibition Assay | IC50=8.17029 μM | SANGER | |||
| AM-38 | Growth Inhibition Assay | IC50=8.1628 μM | SANGER | |||
| NCI-H661 | Growth Inhibition Assay | IC50=8.05867 μM | SANGER | |||
| SHP-77 | Growth Inhibition Assay | IC50=7.86653 μM | SANGER | |||
| DK-MG | Growth Inhibition Assay | IC50=7.83201 μM | SANGER | |||
| NB13 | Growth Inhibition Assay | IC50=7.82667 μM | SANGER | |||
| COLO-829 | Growth Inhibition Assay | IC50=7.66463 μM | SANGER | |||
| OS-RC-2 | Growth Inhibition Assay | IC50=7.49894 μM | SANGER | |||
| HCC1419 | Growth Inhibition Assay | IC50=7.46833 μM | SANGER | |||
| SKG-IIIa | Growth Inhibition Assay | IC50=7.45381 μM | SANGER | |||
| COLO-668 | Growth Inhibition Assay | IC50=7.43967 μM | SANGER | |||
| CAL-62 | Growth Inhibition Assay | IC50=7.39866 μM | SANGER | |||
| HEL | Growth Inhibition Assay | IC50=7.37521 μM | SANGER | |||
| NCI-H2030 | Growth Inhibition Assay | IC50=7.33698 μM | SANGER | |||
| DMS-114 | Growth Inhibition Assay | IC50=7.29631 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=7.25828 μM | SANGER | |||
| KP-N-YS | Growth Inhibition Assay | IC50=7.1814 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=7.1535 μM | SANGER | |||
| NCI-H2405 | Growth Inhibition Assay | IC50=7.08393 μM | SANGER | |||
| TE-11 | Growth Inhibition Assay | IC50=7.04967 μM | SANGER | |||
| KLE | Growth Inhibition Assay | IC50=6.96516 μM | SANGER | |||
| A388 | Growth Inhibition Assay | IC50=6.8952 μM | SANGER | |||
| NB12 | Growth Inhibition Assay | IC50=6.78404 μM | SANGER | |||
| PFSK-1 | Growth Inhibition Assay | IC50=6.73478 μM | SANGER | |||
| SK-HEP-1 | Growth Inhibition Assay | IC50=6.71753 μM | SANGER | |||
| Calu-3 | Growth Inhibition Assay | IC50=6.65568 μM | SANGER | |||
| SH-4 | Growth Inhibition Assay | IC50=6.58844 μM | SANGER | |||
| GCT | Growth Inhibition Assay | IC50=6.53387 μM | SANGER | |||
| MSTO-221H | Growth Inhibition Assay | IC50=6.5117 μM | SANGER | |||
| GAMG | Growth Inhibition Assay | IC50=6.5062 μM | SANGER | |||
| CAL-120 | Growth Inhibition Assay | IC50=6.45162 μM | SANGER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=6.30462 μM | SANGER | |||
| SK-MEL-28 | Growth Inhibition Assay | IC50=6.20967 μM | SANGER | |||
| 8-MG-BA | Growth Inhibition Assay | IC50=6.19379 μM | SANGER | |||
| L-428 | Growth Inhibition Assay | IC50=6.18037 μM | SANGER | |||
| Mewo | Growth Inhibition Assay | IC50=6.11487 μM | SANGER | |||
| RCM-1 | Growth Inhibition Assay | IC50=6.07719 μM | SANGER | |||
| KE-37 | Growth Inhibition Assay | IC50=6.07258 μM | SANGER | |||
| TE-10 | Growth Inhibition Assay | IC50=6.04833 μM | SANGER | |||
| HDLM-2 | Growth Inhibition Assay | IC50=6.01489 μM | SANGER | |||
| CAKI-1 | Growth Inhibition Assay | IC50=6.00985 μM | SANGER | |||
| RT-112 | Growth Inhibition Assay | IC50=5.90245 μM | SANGER | |||
| HCC2998 | Growth Inhibition Assay | IC50=5.71877 μM | SANGER | |||
| HCC1187 | Growth Inhibition Assay | IC50=5.71032 μM | SANGER | |||
| HD-MY-Z | Growth Inhibition Assay | IC50=5.68581 μM | SANGER | |||
| RMG-I | Growth Inhibition Assay | IC50=5.65942 μM | SANGER | |||
| BFTC-905 | Growth Inhibition Assay | IC50=5.65878 μM | SANGER | |||
| SW1990 | Growth Inhibition Assay | IC50=5.62285 μM | SANGER | |||
| SW13 | Growth Inhibition Assay | IC50=5.53265 μM | SANGER | |||
| AGS | Growth Inhibition Assay | IC50=5.49618 μM | SANGER | |||
| ATN-1 | Growth Inhibition Assay | IC50=5.41184 μM | SANGER | |||
| CGTH-W-1 | Growth Inhibition Assay | IC50=5.38584 μM | SANGER | |||
| NOMO-1 | Growth Inhibition Assay | IC50=5.23176 μM | SANGER | |||
| ALL-PO | Growth Inhibition Assay | IC50=5.22587 μM | SANGER | |||
| KP-N-YN | Growth Inhibition Assay | IC50=5.12591 μM | SANGER | |||
| NCI-H1838 | Growth Inhibition Assay | IC50=5.02076 μM | SANGER | |||
| TE-9 | Growth Inhibition Assay | IC50=5.01525 μM | SANGER | |||
| KOSC-2 | Growth Inhibition Assay | IC50=4.99959 μM | SANGER | |||
| ES1 | Growth Inhibition Assay | IC50=4.96035 μM | SANGER | |||
| KNS-62 | Growth Inhibition Assay | IC50=4.90807 μM | SANGER | |||
| KYSE-520 | Growth Inhibition Assay | IC50=4.88018 μM | SANGER | |||
| P30-OHK | Growth Inhibition Assay | IC50=4.81929 μM | SANGER | |||
| NB10 | Growth Inhibition Assay | IC50=4.59781 μM | SANGER | |||
| A172 | Growth Inhibition Assay | IC50=4.55521 μM | SANGER | |||
| SK-OV-3 | Growth Inhibition Assay | IC50=4.46042 μM | SANGER | |||
| GR-ST | Growth Inhibition Assay | IC50=4.4318 μM | SANGER | |||
| HCC1937 | Growth Inhibition Assay | IC50=4.37993 μM | SANGER | |||
| LU-139 | Growth Inhibition Assay | IC50=4.37247 μM | SANGER | |||
| SNU-C2B | Growth Inhibition Assay | IC50=4.34686 μM | SANGER | |||
| KARPAS-299 | Growth Inhibition Assay | IC50=4.31013 μM | SANGER | |||
| EW-11 | Growth Inhibition Assay | IC50=4.13261 μM | SANGER | |||
| HL-60 | Growth Inhibition Assay | IC50=4.12241 μM | SANGER | |||
| TCCSUP | Growth Inhibition Assay | IC50=4.1105 μM | SANGER | |||
| RCC10RGB | Growth Inhibition Assay | IC50=4.01246 μM | SANGER | |||
| NCI-H441 | Growth Inhibition Assay | IC50=3.97014 μM | SANGER | |||
| EW-16 | Growth Inhibition Assay | IC50=3.95577 μM | SANGER | |||
| JVM-2 | Growth Inhibition Assay | IC50=3.94752 μM | SANGER | |||
| NH-12 | Growth Inhibition Assay | IC50=3.94187 μM | SANGER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=3.94029 μM | SANGER | |||
| NCI-H69 | Growth Inhibition Assay | IC50=3.90178 μM | SANGER | |||
| KURAMOCHI | Growth Inhibition Assay | IC50=3.86056 μM | SANGER | |||
| NCI-H1155 | Growth Inhibition Assay | IC50=3.84159 μM | SANGER | |||
| NCI-H28 | Growth Inhibition Assay | IC50=3.82961 μM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=3.82286 μM | SANGER | |||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=3.75406 μM | SANGER | |||
| PANC-10-05 | Growth Inhibition Assay | IC50=3.72072 μM | SANGER | |||
| SK-MES-1 | Growth Inhibition Assay | IC50=3.64614 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=3.64407 μM | SANGER | |||
| A2780 | Growth Inhibition Assay | IC50=3.64089 μM | SANGER | |||
| CaR-1 | Growth Inhibition Assay | IC50=3.61048 μM | SANGER | |||
| SK-LU-1 | Growth Inhibition Assay | IC50=3.60645 μM | SANGER | |||
| OAW-28 | Growth Inhibition Assay | IC50=3.59426 μM | SANGER | |||
| TE-1 | Growth Inhibition Assay | IC50=3.59169 μM | SANGER | |||
| 639-V | Growth Inhibition Assay | IC50=3.57792 μM | SANGER | |||
| C8166 | Growth Inhibition Assay | IC50=3.46521 μM | SANGER | |||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=3.44957 μM | SANGER | |||
| D-542MG | Growth Inhibition Assay | IC50=3.44222 μM | SANGER | |||
| LB771-HNC | Growth Inhibition Assay | IC50=3.39126 μM | SANGER | |||
| NCI-H727 | Growth Inhibition Assay | IC50=3.38584 μM | SANGER | |||
| SW1463 | Growth Inhibition Assay | IC50=3.26192 μM | SANGER | |||
| NCI-H1793 | Growth Inhibition Assay | IC50=3.21098 μM | SANGER | |||
| HT-1376 | Growth Inhibition Assay | IC50=3.20506 μM | SANGER | |||
| 647-V | Growth Inhibition Assay | IC50=3.1622 μM | SANGER | |||
| BCPAP | Growth Inhibition Assay | IC50=3.08295 μM | SANGER | |||
| MN-60 | Growth Inhibition Assay | IC50=3.04974 μM | SANGER | |||
| COLO-680N | Growth Inhibition Assay | IC50=3.00495 μM | SANGER | |||
| DU-4475 | Growth Inhibition Assay | IC50=2.99052 μM | SANGER | |||
| NCI-H1693 | Growth Inhibition Assay | IC50=2.95897 μM | SANGER | |||
| HC-1 | Growth Inhibition Assay | IC50=2.94012 μM | SANGER | |||
| KYSE-510 | Growth Inhibition Assay | IC50=2.86786 μM | SANGER | |||
| OVCAR-3 | Growth Inhibition Assay | IC50=2.85594 μM | SANGER | |||
| PC-3 | Growth Inhibition Assay | IC50=2.83317 μM | SANGER | |||
| BB65-RCC | Growth Inhibition Assay | IC50=2.80713 μM | SANGER | |||
| QIMR-WIL | Growth Inhibition Assay | IC50=2.75952 μM | SANGER | |||
| HuP-T4 | Growth Inhibition Assay | IC50=2.72818 μM | SANGER | |||
| Detroit562 | Growth Inhibition Assay | IC50=2.69845 μM | SANGER | |||
| DMS-79 | Growth Inhibition Assay | IC50=2.69284 μM | SANGER | |||
| MC-IXC | Growth Inhibition Assay | IC50=2.64453 μM | SANGER | |||
| TE-8 | Growth Inhibition Assay | IC50=2.63653 μM | SANGER | |||
| MKN7 | Growth Inhibition Assay | IC50=2.62748 μM | SANGER | |||
| HH | Growth Inhibition Assay | IC50=2.49854 μM | SANGER | |||
| CFPAC-1 | Growth Inhibition Assay | IC50=2.43864 μM | SANGER | |||
| HTC-C3 | Growth Inhibition Assay | IC50=2.42267 μM | SANGER | |||
| NY | Growth Inhibition Assay | IC50=2.3727 μM | SANGER | |||
| KU812 | Growth Inhibition Assay | IC50=2.36779 μM | SANGER | |||
| EW-18 | Growth Inhibition Assay | IC50=2.35471 μM | SANGER | |||
| NCI-H2170 | Growth Inhibition Assay | IC50=2.34783 μM | SANGER | |||
| JVM-3 | Growth Inhibition Assay | IC50=2.34643 μM | SANGER | |||
| IGROV-1 | Growth Inhibition Assay | IC50=2.31237 μM | SANGER | |||
| A498 | Growth Inhibition Assay | IC50=2.29415 μM | SANGER | |||
| BT-20 | Growth Inhibition Assay | IC50=2.26744 μM | SANGER | |||
| SCC-4 | Growth Inhibition Assay | IC50=2.21776 μM | SANGER | |||
| 786-0 | Growth Inhibition Assay | IC50=2.18406 μM | SANGER | |||
| RXF393 | Growth Inhibition Assay | IC50=2.13036 μM | SANGER | |||
| KARPAS-45 | Growth Inhibition Assay | IC50=2.12479 μM | SANGER | |||
| RPMI-8866 | Growth Inhibition Assay | IC50=2.08481 μM | SANGER | |||
| NCI-H2009 | Growth Inhibition Assay | IC50=2.06214 μM | SANGER | |||
| SW1116 | Growth Inhibition Assay | IC50=2.06009 μM | SANGER | |||
| EKVX | Growth Inhibition Assay | IC50=2.04939 μM | SANGER | |||
| TGBC24TKB | Growth Inhibition Assay | IC50=2.02961 μM | SANGER | |||
| CAL-12T | Growth Inhibition Assay | IC50=2.01861 μM | SANGER | |||
| HCC70 | Growth Inhibition Assay | IC50=2.00815 μM | SANGER | |||
| OMC-1 | Growth Inhibition Assay | IC50=1.99888 μM | SANGER | |||
| EPLC-272H | Growth Inhibition Assay | IC50=1.85549 μM | SANGER | |||
| NCI-H209 | Growth Inhibition Assay | IC50=1.77269 μM | SANGER | |||
| NCI-H1666 | Growth Inhibition Assay | IC50=1.74704 μM | SANGER | |||
| COLO-678 | Growth Inhibition Assay | IC50=1.73444 μM | SANGER | |||
| PANC-03-27 | Growth Inhibition Assay | IC50=1.70139 μM | SANGER | |||
| BB30-HNC | Growth Inhibition Assay | IC50=1.68972 μM | SANGER | |||
| ML-2 | Growth Inhibition Assay | IC50=1.64029 μM | SANGER | |||
| BT-549 | Growth Inhibition Assay | IC50=1.58747 μM | SANGER | |||
| HSC-3 | Growth Inhibition Assay | IC50=1.5438 μM | SANGER | |||
| LAMA-84 | Growth Inhibition Assay | IC50=1.53815 μM | SANGER | |||
| SCC-25 | Growth Inhibition Assay | IC50=1.52322 μM | SANGER | |||
| SAS | Growth Inhibition Assay | IC50=1.51622 μM | SANGER | |||
| BE-13 | Growth Inhibition Assay | IC50=1.50671 μM | SANGER | |||
| J82 | Growth Inhibition Assay | IC50=1.45766 μM | SANGER | |||
| 697 | Growth Inhibition Assay | IC50=1.44104 μM | SANGER | |||
| NCI-H526 | Growth Inhibition Assay | IC50=1.43826 μM | SANGER | |||
| RH-1 | Growth Inhibition Assay | IC50=1.41136 μM | SANGER | |||
| CCRF-CEM | Growth Inhibition Assay | IC50=1.4111 μM | SANGER | |||
| NB5 | Growth Inhibition Assay | IC50=1.40894 μM | SANGER | |||
| KMOE-2 | Growth Inhibition Assay | IC50=1.39815 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=1.36947 μM | SANGER | |||
| SW48 | Growth Inhibition Assay | IC50=1.36618 μM | SANGER | |||
| SW954 | Growth Inhibition Assay | IC50=1.34048 μM | SANGER | |||
| NCI-H1650 | Growth Inhibition Assay | IC50=1.33482 μM | SANGER | |||
| NKM-1 | Growth Inhibition Assay | IC50=1.32597 μM | SANGER | |||
| NCI-H1092 | Growth Inhibition Assay | IC50=1.3085 μM | SANGER | |||
| CTV-1 | Growth Inhibition Assay | IC50=1.308 μM | SANGER | |||
| GCIY | Growth Inhibition Assay | IC50=1.30132 μM | SANGER | |||
| SW1088 | Growth Inhibition Assay | IC50=1.29607 μM | SANGER | |||
| 769-P | Growth Inhibition Assay | IC50=1.27918 μM | SANGER | |||
| OAW-42 | Growth Inhibition Assay | IC50=1.27825 μM | SANGER | |||
| SNU-449 | Growth Inhibition Assay | IC50=1.22208 μM | SANGER | |||
| MKN1 | Growth Inhibition Assay | IC50=1.21987 μM | SANGER | |||
| NCI-H1648 | Growth Inhibition Assay | IC50=1.10616 μM | SANGER | |||
| KU-19-19 | Growth Inhibition Assay | IC50=1.08541 μM | SANGER | |||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=1.08451 μM | SANGER | |||
| EM-2 | Growth Inhibition Assay | IC50=1.03016 μM | SANGER | |||
| NCI-H1304 | Growth Inhibition Assay | IC50=1.01643 μM | SANGER | |||
| DOHH-2 | Growth Inhibition Assay | IC50=1.00021 μM | SANGER | |||
| MS-1 | Growth Inhibition Assay | IC50=994.69 nM | SANGER | |||
| SK-NEP-1 | Growth Inhibition Assay | IC50=989.44 nM | SANGER | |||
| HT-3 | Growth Inhibition Assay | IC50=982.41 nM | SANGER | |||
| BHY | Growth Inhibition Assay | IC50=975.48 nM | SANGER | |||
| BT-474 | Growth Inhibition Assay | IC50=938.14 nM | SANGER | |||
| CAPAN-1 | Growth Inhibition Assay | IC50=883.29 nM | SANGER | |||
| NCI-H2126 | Growth Inhibition Assay | IC50=882.83 nM | SANGER | |||
| COR-L88 | Growth Inhibition Assay | IC50=882.26 nM | SANGER | |||
| DEL | Growth Inhibition Assay | IC50=877.65 nM | SANGER | |||
| AU565 | Growth Inhibition Assay | IC50=869.6 nM | SANGER | |||
| 23132-87 | Growth Inhibition Assay | IC50=864.28 nM | SANGER | |||
| LoVo | Growth Inhibition Assay | IC50=859.06 nM | SANGER | |||
| TE-12 | Growth Inhibition Assay | IC50=821.11 nM | SANGER | |||
| EC-GI-10 | Growth Inhibition Assay | IC50=788.52 nM | SANGER | |||
| LU-135 | Growth Inhibition Assay | IC50=783.03 nM | SANGER | |||
| A431 | Growth Inhibition Assay | IC50=780.04 nM | SANGER | |||
| TE-6 | Growth Inhibition Assay | IC50=764.31 nM | SANGER | |||
| COLO-684 | Growth Inhibition Assay | IC50=753.01 nM | SANGER | |||
| HAL-01 | Growth Inhibition Assay | IC50=734.71 nM | SANGER | |||
| NCI-H1770 | Growth Inhibition Assay | IC50=722.4 nM | SANGER | |||
| LU-134-A | Growth Inhibition Assay | IC50=719.09 nM | SANGER | |||
| L-363 | Growth Inhibition Assay | IC50=671.94 nM | SANGER | |||
| ETK-1 | Growth Inhibition Assay | IC50=662.59 nM | SANGER | |||
| COR-L105 | Growth Inhibition Assay | IC50=662.53 nM | SANGER | |||
| NBsusSR | Growth Inhibition Assay | IC50=646.52 nM | SANGER | |||
| ME-180 | Growth Inhibition Assay | IC50=632.9 nM | SANGER | |||
| DBTRG-05MG | Growth Inhibition Assay | IC50=632.28 nM | SANGER | |||
| MV-4-11 | Growth Inhibition Assay | IC50=627.7 nM | SANGER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=625.29 nM | SANGER | |||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=621.46 nM | SANGER | |||
| NB69 | Growth Inhibition Assay | IC50=614.35 nM | SANGER | |||
| FADU | Growth Inhibition Assay | IC50=604.69 nM | SANGER | |||
| NCI-H1623 | Growth Inhibition Assay | IC50=599.36 nM | SANGER | |||
| CAL-39 | Growth Inhibition Assay | IC50=596.3 nM | SANGER | |||
| Ca9-22 | Growth Inhibition Assay | IC50=588.64 nM | SANGER | |||
| CAN | Growth Inhibition Assay | IC50=580.76 nM | SANGER | |||
| RS4-11 | Growth Inhibition Assay | IC50=568.59 nM | SANGER | |||
| DSH1 | Growth Inhibition Assay | IC50=566.88 nM | SANGER | |||
| NB7 | Growth Inhibition Assay | IC50=546.32 nM | SANGER | |||
| NCI-H82 | Growth Inhibition Assay | IC50=540.5 nM | SANGER | |||
| KYSE-180 | Growth Inhibition Assay | IC50=530.62 nM | SANGER | |||
| NCI-H358 | Growth Inhibition Assay | IC50=527.66 nM | SANGER | |||
| SCC-15 | Growth Inhibition Assay | IC50=525.68 nM | SANGER | |||
| HN | Growth Inhibition Assay | IC50=517.38 nM | SANGER | |||
| TK10 | Growth Inhibition Assay | IC50=515.11 nM | SANGER | |||
| MOLT-13 | Growth Inhibition Assay | IC50=514.82 nM | SANGER | |||
| SK-MEL-1 | Growth Inhibition Assay | IC50=510.99 nM | SANGER | |||
| HO-1-N-1 | Growth Inhibition Assay | IC50=509.25 nM | SANGER | |||
| KYSE-270 | Growth Inhibition Assay | IC50=498.65 nM | SANGER | |||
| BPH-1 | Growth Inhibition Assay | IC50=491.16 nM | SANGER | |||
| EFO-27 | Growth Inhibition Assay | IC50=454.74 nM | SANGER | |||
| DoTc2-4510 | Growth Inhibition Assay | IC50=442.12 nM | SANGER | |||
| CTB-1 | Growth Inhibition Assay | IC50=424.4 nM | SANGER | |||
| KY821 | Growth Inhibition Assay | IC50=408.57 nM | SANGER | |||
| NUGC-3 | Growth Inhibition Assay | IC50=401.81 nM | SANGER | |||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=378.88 nM | SANGER | |||
| CAL-33 | Growth Inhibition Assay | IC50=370.9 nM | SANGER | |||
| KASUMI-1 | Growth Inhibition Assay | IC50=366.73 nM | SANGER | |||
| ECC10 | Growth Inhibition Assay | IC50=352.96 nM | SANGER | |||
| A4-Fuk | Growth Inhibition Assay | IC50=350.02 nM | SANGER | |||
| SK-MEL-24 | Growth Inhibition Assay | IC50=337.87 nM | SANGER | |||
| HCC1806 | Growth Inhibition Assay | IC50=337.51 nM | SANGER | |||
| PC-14 | Growth Inhibition Assay | IC50=333.41 nM | SANGER | |||
| ACHN | Growth Inhibition Assay | IC50=331.4 nM | SANGER | |||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=328.06 nM | SANGER | |||
| TI-73 | Growth Inhibition Assay | IC50=312.75 nM | SANGER | |||
| CAL-54 | Growth Inhibition Assay | IC50=311.23 nM | SANGER | |||
| SBC-1 | Growth Inhibition Assay | IC50=307.79 nM | SANGER | |||
| BALL-1 | Growth Inhibition Assay | IC50=297.42 nM | SANGER | |||
| CAL-27 | Growth Inhibition Assay | IC50=289.08 nM | SANGER | |||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=283.32 nM | SANGER | |||
| HCE-T | Growth Inhibition Assay | IC50=279.79 nM | SANGER | |||
| MEG-01 | Growth Inhibition Assay | IC50=276.76 nM | SANGER | |||
| CAL-72 | Growth Inhibition Assay | IC50=268.73 nM | SANGER | |||
| KYSE-450 | Growth Inhibition Assay | IC50=247.92 nM | SANGER | |||
| EW-13 | Growth Inhibition Assay | IC50=225.1 nM | SANGER | |||
| DU-145 | Growth Inhibition Assay | IC50=219.04 nM | SANGER | |||
| KYSE-140 | Growth Inhibition Assay | IC50=209.96 nM | SANGER | |||
| CHL-1 | Growth Inhibition Assay | IC50=208.51 nM | SANGER | |||
| KG-1 | Growth Inhibition Assay | IC50=204.34 nM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=194.93 nM | SANGER | |||
| BV-173 | Growth Inhibition Assay | IC50=186.55 nM | SANGER | |||
| LU-65 | Growth Inhibition Assay | IC50=166.61 nM | SANGER | |||
| HSC-2 | Growth Inhibition Assay | IC50=165.57 nM | SANGER | |||
| NCI-H292 | Growth Inhibition Assay | IC50=162.66 nM | SANGER | |||
| H9 | Growth Inhibition Assay | IC50=137.2 nM | SANGER | |||
| DOK | Growth Inhibition Assay | IC50=93.62 nM | SANGER | |||
| HSC-4 | Growth Inhibition Assay | IC50=61.53 nM | SANGER | |||
| DB | Growth Inhibition Assay | IC50=60.96 nM | SANGER | |||
| HuO-3N1 | Growth Inhibition Assay | IC50=56.09 nM | SANGER | |||
| HCC2218 | Growth Inhibition Assay | IC50=50.59 nM | SANGER | |||
| EW-3 | Growth Inhibition Assay | IC50=46.04 nM | SANGER | |||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=28.19 nM | SANGER | |||
| NCI-H720 | Growth Inhibition Assay | IC50=26.92 nM | SANGER | |||
| EoL-1 | Growth Inhibition Assay | IC50=5.17 nM | SANGER | |||
| MIAPaCa2 | Apoptosis Assay | 20 μM | 24 h | DMSO | does not induce apoptosis assessed as caspase 3 activation | 20466555 |
| MIAPaCa2 | Apoptosis Assay | 10 μM | 24h or 48 h | DMSO | does not induce apoptosis | 20466555 |
| MIAPaCa2 | Cytotoxic Assay | 1 μM | 10 d | DMSO | has no cytotoxicity assessed as suppression of colony formation | 20466555 |
| MIAPaCa2 | Growth Inhibition Assay | 2.5 μM | 72 h | DMSO | has no growth inhibition | 20466555 |
| H1975 | Kinase Assay | 0.5 μM | 24 h | DMSO | does not inhibit EGFR L858R/T790M mutant-mediated Akt phosphorylation | 22339342 |
| H1975 | Kinase Assay | 0.5 μM | 24 h | DMSO | does not inhibit EGFR L858R/T790M mutant-mediated Erk phosphorylation | 22339342 |
| H1975 | Kinase Assay | 0.125 μM | 24 h | DMSO | does not inhibit EGFR L858R/T790M mutant Y1068 autophosphorylation | 22339342 |
| H1975 | Kinase Assay | 0.33 μM | 2 h | DMSO | does not inhibit EGFR L858R/T790M double mutant phosphorylation | 24124898 |
| H1975 | Kinase Assay | 0.33 μM | 2 h | DMSO | does not inhibit EGFR L858R/T790M double mutant assessed as reduction in ERK phosphorylation | 24124898 |
| H1975 | Kinase Assay | 0.33 μM | 2 h | DMSO | does not inhibit EGFR L858R/T790M double mutant assessed as reduction in AKT phosphorylation | 24124898 |
| HCC827 | Kinase Assay | 0.11 μM | 1 h | DMSO | has no irreversible inhibition of EGFR assessed as recovery of EGFR autophosphorylation | 24124898 |
| H1975 | Function Assay | 1 μM | 24 h | DMSO | does not inhibit ERK phosphorylation in human H1975 cells harboring EGFR L858R/T790M | 24607591 |
| H1975 | Kinase Assay | 1 μM | 24 h | DMSO | does not inhibit EGFR phosphorylation in human H1975 cells harboring EGFR L858R/T790M mutant | 24607591 |
| LNCaP | Function Assay | 10 μM | 2h or 4 h | DMSO | does not inhibit autophosphorylation of immunopurified flag-tagged Bmx assessed as incorporation of [32P]ATP | 18667312 |
| A431 | Kinase Assay | 1 μM | 1 h | DMSO | has no irreversible inhibition of EGFR autophosphorylation | 24900594 |
| NCI-H1975 | Function Assay | 10 μM | 8 h | DMSO | does not inhibiti EGFR assessed as reduction in ERK phosphorylation | 23116168 |
| HCC827 | Cytotoxic Assay | 0.5 μM | 72 h | DMSO | has no cytotoxicity | 23993328 |
| HCC827 | Function Assay | 0.5 μM | 2 h | DMSO | does not inhibit c-Met assessed as inhibition of p44/42 phosphorylation | 23993328 |
| HCC827 | Function Assay | 0.5 μM | 2 h | DMSO | does not inhibit c-Met assessed as inhibition of AKT phosphorylation | 23993328 |
| SW620 | Cytotoxic Assay | 48 h | DMSO | IC50=28.2 μM | 24900594 | |
| Sf9 | Kinase Assay | 10 min | DMSO | Inhibition of autophosphorylation of recombinant his-tagged EGFR (amino acid 645-1186) expressed with IC50 of 0.02 μM | 24731281 | |
| HepG2 | Growth Inhibition Assay | 24 h | DMSO | IC50=6.42 μM | 24731281 | |
| Hela | Growth Inhibition Assay | 24 h | DMSO | IC50=2.67 μM | 24731281 | |
| NCI-H1975 | Function Assay | 100 μM | 150 min | DMSO | Induction of NO production in human NCI-H1975 cells harboring EGFR L858R/T790M mutant | 24607591 |
| BEAS2B | Growth Inhibition Assay | 50 μM | 72 h | DMSO | IC50=13.94 μM | 24607591 |
| KB | Kinase Assay | 10 μM | 1 h | DMSO | Inhibition of EGF-stimulated autophosphorylation of EGFR with IC50 of 0.025 μM | 24411123 |
| Calu3 | Cytotoxic Assay | 72 h | DMSO | Cytotoxicity against human Calu3 cells expressing HER2 with IC50 of 0.99 μM | 24411123 | |
| A431 | Cytotoxic Assay | 72 h | DMSO | Cytotoxicity against human A431 cells expressing EGFR with IC50 of 0.55 μM | 24411123 | |
| MDCK2 | Function Assay | 1.8 μM | 72 h | DMSO | Inhibition of human BCRP expressed assessed as Hoechst 33342 accumulation with IC50 of 3.19 μM | 24184213 |
| MDCK | Cytotoxic Assay | 72 h | DMSO | GI50=1.45 μM | 24184213 | |
| BCRP-MDCK2 | Function Assay | 1.8 μM | 72 h | DMSO | Reduction of plasma membrane expression of BCRP expressing reporter gene GFP | 24184213 |
| BCRP-MDCK2 | Function Assay | 1.8 μM | 72 h | DMSO | Increase of plasma membrane expression of BCRP expressing reporter gene GFP | 24184213 |
| A431 | Kinase Assay | 100 μM | 30 min | Inhibition of EGFR in shed membrane vesicles with IC50 of 1.1 μM | 24094432 | |
| HCC827 | Growth Inhibition Assay | 10 μM | 72 h | DMSO | Antiproliferative activity against gefitinib-sensitive human HCC827 cells harboring EGFR E746 to A750 deletion with IC50 of 0.00581 μM | 24053674 |
| HCC827 | Function Assay | 0.5 μM | 2 h | DMSO | Inhibition of c-Met phosphorylation in gefitinib-resistant human HCC827 cells | 23993328 |
| HCC827 | Kinase Assay | 0.5 μM | 2 h | DMSO | Inhibition of EGFR phosphorylation in gefitinib-resistant human HCC827 cells | 23993328 |
| A549 | Function Assay | 1 μM | 1 h | DMSO | Cellular uptake | 23988354 |
| A549 | Kinase Assay | 1 μM | 1 h | DMSO | Inhibition of EGFR autophosphorylation with IC50 of 0.0399 μM | 23988354 |
| HCC827 | Growth Inhibition Assay | 72 h | IC50=0.012 μM | 23973168 | ||
| PC9 | Kinase Assay | 2 h | DMSO | Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells with IC50 of 0.0087 μM | 23930994 | |
| LoVo | Kinase Assay | 2 h | DMSO | Inhibition of EGFR phosphorylation with IC50 of 0.062 μM | 23930994 | |
| SH-SY5Y | Cytotoxic Assay | 72 h | IC50=18.21 μM | 23871909 | ||
| A549 | Growth Inhibition Assay | 72 h | DMSO | Antiproliferative activity against wild type EGFR/k-Ras dependent human A549 cells with IC50 of 4.626 μM | 23792318 | |
| 16HBE | Function Assay | 100 μM | 150 min | DMSO | Induction of nitric oxide production in human 16HBE cells expressing wild type EGFR | 23792318 |
| 16HBE | Growth Inhibition Assay | 72 h | DMSO | Antiproliferative activity against human 16HBE cells expressing wild type EGFR with IC50 of 1.601 μM | 23792318 | |
| NCI-H1975 | Cytotoxic Assay | 10 μM | 72 h | DMSO | Cytotoxicity against gefitinib-resistant human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition with IC50 of 6.917 μM | 23668441 |
| 16HBE14o- | Cytotoxic Assay | 10 μM | 72 h | DMSO | Cytotoxicity against human 16HBE14o- cells harboring wild type EGFR assessed as growth inhibition with IC50 of 12.71 μM | 23668441 |
| Sf9 | Kinase Assay | 1 h | DMSO | Inhibition of human GST-tagged EGFR L834R mutant expressed with IC50 of 0.015 μM | 23611691 | |
| PC9 | Growth Inhibition Assay | 10 μg/mL | 72 h | IC50=0.014 μM | 23116168 | |
| HCC827 | Cytotoxic Assay | 10 μg/mL | 72 h | IC50=0.0015 μM | 23116168 | |
| FADU | Cytotoxic Assay | 10 μg/mL | 72 h | IC50=0.05 μM | 23116168 | |
| Calu3 | Cytotoxic Assay | 10 μg/mL | 72 h | IC50=1.6 μM | 23116168 | |
| A498 | Growth Inhibition Assay | Antiproliferative activity against human A498 cells expressing EGFR and SRC with IC50 of 8.6 μM | 22818848 | |||
| SGC7901 | Cytotoxic Assay | 72 h | IC50=10.26 μM | 22727449 | ||
| HT-29 | Cytotoxic Assay | 72 h | IC50=3.36 μM | 22727449 | ||
| H460 | Cytotoxic Assay | 72 h | IC50=5.59 μM | 22727449 | ||
| A431 | Kinase Assay | 100 μM | 30 min | Inhibition of EGFR derived from human A431 cell membrane assessed as inhibition of poly-Glu-Tyr phosphorylation with IC50 of 1.08 μM | 22698782 | |
| HCC827 | Kinase Assay | 0.125 μM | 24 h | DMSO | Inhibition of EGFR del E746-A750 mutant-mediated Akt phosphorylation | 22339342 |
| HCC827 | Kinase Assay | 0.125 μM | 24 h | DMSO | Inhibition of EGFR del E746-A750 mutant-mediated Erk phosphorylation | 22339342 |
| HCC827 | Kinase Assay | 0.125 μM | 24 h | DMSO | Inhibition of EGFR del E746-A750 mutant Y1068 autophosphorylation | 22339342 |
| MCF7 | Cytotoxic Assay | 10 μM | 48 h | Cytotoxicity against serum-starved human MCF7 cells over-expressing ErbB2 cells | 22138308 | |
| BT474 | Cytotoxic Assay | 10 μM | 48 h | Cytotoxicity against serum-starved human BT474 cells | 22138308 | |
| MCF7 | Growth Inhibition Assay | 100 μg/mL | 48 h | DMSO | Antiproliferative activity against human MCF7 cells overexpressing EGFR gene with IC50 of 12.05 μM | 22119130 |
| A431 | Kinase Assay | 2 h | DMSO | Inhibition of EGFR phosphorylation in EGF-stimulated human A431 with IC50 of 0.001 μM | 22101132 | |
| NCI-H292 | Growth Inhibition Assay | 72 h | DMSO | IC50=0.02 μM | 21916433 | |
| NCI-H1993 | Growth Inhibition Assay | 72 h | DMSO | IC50=0.1 μM | 21916433 | |
| Plasmodium falciparum | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 21817045 | ||||
| MDA-MB-468 | Growth Inhibition Assay | 100 μM | 48 h | DMSO | Antiproliferative activity | 21429632 |
| PC3 | Growth Inhibition Assay | 10 μM | 72 h | DMSO | IC50=7.4 μM | 21353546 |
| PC9 | Growth Inhibition Assay | Antiproliferative activity against growth-resistant human PC9 cells expressing EGFR E746_A750/T790M mutant with EC50 of 7 μM | 21208802 | |||
| PC9 | Growth Inhibition Assay | Antiproliferative activity against EGFR-deficient human PC9 cells with EC50 of 0.017 μM | 21208802 | |||
| PANC1 | Cytotoxic Assay | 5 d | DMSO | IC50=40.42 μM | 20466555 | |
| MIAPaCa2 | Cytotoxic Assay | 5 d | DMSO | IC50=50.62 μM | 20466555 | |
| DU145 | Cytotoxic Assay | 5 d | DMSO | IC50=42.17 μM | 20466555 | |
| SMMC7721 | Growth Inhibition Assay | 48 h | IC50=33.12 μM | 20304537 | ||
| A375 | Growth Inhibition Assay | 48 h | IC50=20.55 μM | 20304537 | ||
| NCI-H1975 | Function Assay | 5 μM | 48 h | Induction of apoptosis assessed as activation of caspase-3 | 20151670 | |
| NCI-H1975 | Function Assay | 10 μM | Inhibition of ERBB2 autophosphorylation | 20151670 | ||
| NCI-H1975 | Kinase Assay | 10 μM | Inhibition of EGFR autophosphorylation | 20151670 | ||
| NCI-H1975 | Growth Inhibition Assay | 5 μM | 72 h | IC50=8.26 μM | 20151670 | |
| Sf9 | Kinase Assay | 10 min | DMSO | Inhibition of EGFR expressed assessed as inhibition of receptor autophosphorylation with IC50 of 0.033 μM | 20056425 | |
| A431 | Kinase Assay | 100 μM | 10 min | Prolonged inhibitory activity of EGF-induced EGFR phosphorylation | 19969465 | |
| A431 | Kinase Assay | 0.1 μM | 1 h | Inhibition of EGF-induced EGFR phosphorylation | 19969465 | |
| A431 | Growth Inhibition Assay | 10 μM | 72 h | GI50=0.514 μM | 19969465 | |
| MCF7 MX | Function Assay | 30 min | Inhibition of BCRP expressed with IC50 of 1.1 μM | 19932960 | ||
| NIH3T3 | Growth Inhibition Assay | 72 h | Growth inhibition of mouse NIH/3T3 cells expressing erB2 gene with IC50 of 0.54 μM | 19665377 | ||
| BA/F3 | Cytotoxic Assay | 72 h | Cytotoxicity against mouse BA/F3 cells expressing EGFR L858R mutant with IC50 of 0.0108 μM | 19239229 | ||
| HN5 | Growth Inhibition Assay | 72 h | Antiproliferative activity against human HN5 cells overexpressing EGFR with EC50 of 0.01 μM | 19028424 | ||
| BT474 | Growth Inhibition Assay | 72 h | Antiproliferative activity against human BT474 cells overexpressing ERBb2 with EC50 of 0.3 μM | 19028424 | ||
| MCF7 | Cytotoxic Assay | 50 μM | 72 h | IC50=12.05 μM | 18771819 | |
| MOLT4 | Cytotoxic Assay | 96 h | DMSO | IC50=15.02 μM | 18313807 | |
| MDA-MB-231 | Cytotoxic Assay | 96 h | DMSO | IC50=36.61 μM | 18313807 | |
| K562 | Cytotoxic Assay | 96 h | DMSO | IC50=9.36 μM | 18313807 | |
| A549 | Cytotoxic Assay | 96 h | DMSO | IC50=13.59 μM | 18313807 | |
| COS7 | Function Assay | 96 μM | Inhibition of human JAK2 V617F mutant expressed | 17178722 | ||
| NIH3T3 | Function Assay | 0.2 μM | 2 h | DMSO | Inhibition of EGF stimulated human erbB1 autophosphorylation with IC50 of 0.0144 μM | 16480284 |
| KB | Growth Inhibition Assay | IC50=0.054 μM | 16516473 | |||
| GAK | Growth Inhibition Assay | IC50=21.499 μM | 29795767 | |||
| SK-N-AS | Growth Inhibition Assay | IC50=21.5619 μM | 19691349 | |||
| OE33 | Growth Inhibition Assay | IC50=21.6046 μM | 18469809 | |||
| YKG-1 | Growth Inhibition Assay | IC50=21.6545 μM | 22944119 | |||
| CAL-85 | Growth Inhibition Assay | IC50=21.9305 μM | 24631359 | |||
| NCI-H2347 | Growth Inhibition Assay | IC50=21.9428 μM | 28221790 | |||
| PANC-08-13 | Growth Inhibition Assay | IC50=22.0119 μM | 28221790 | |||
| SK-N-FI | Growth Inhibition Assay | IC50=22.3074 μM | 18469809 | |||
| NEC8 | Growth Inhibition Assay | IC50=22.5078 μM | 22944119 | |||
| AN3-CA | Growth Inhibition Assay | IC50=22.6084 μM | 22944119 | |||
| HuO9 | Growth Inhibition Assay | IC50=22.7396 μM | 27032331 | |||
| COLO-800 | Growth Inhibition Assay | IC50=22.7653 μM | 24341356 | |||
| HT-29 | Growth Inhibition Assay | IC50=22.8823 μM | 21711054 | |||
| OC-314 | Growth Inhibition Assay | IC50=22.8845 μM | 20873740 | |||
| G-401 | Growth Inhibition Assay | IC50=23.0462 μM | 18469809 | |||
| Saos-2 | Growth Inhibition Assay | IC50=23.5182 μM | 24471998 | |||
| UACC-62 | Growth Inhibition Assay | IC50=23.5833 μM | 19691349 | |||
| D-247MG | Growth Inhibition Assay | IC50=23.7939 μM | 18469809 | |||
| COLO-741 | Growth Inhibition Assay | IC50=23.9565 μM | 20580554 | |||
| ES3 | Growth Inhibition Assay | IC50=24.0023 μM | 28221790 | |||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=24.0211 μM | 28221790 | |||
| SW1710 | Growth Inhibition Assay | IC50=24.1506 μM | 23094992 | |||
| LU-99A | Growth Inhibition Assay | IC50=24.1841 μM | 17602464 | |||
| HOP-92 | Growth Inhibition Assay | IC50=24.725 μM | 24471998 | |||
| LS-123 | Growth Inhibition Assay | IC50=24.9614 μM | 22342146 | |||
| T84 | Growth Inhibition Assay | IC50=24.9765 μM | 29328656 | |||
| HCT-116 | Growth Inhibition Assay | IC50=25.4186 μM | 29471119 | |||
| M14 | Growth Inhibition Assay | IC50=25.4447 μM | 17602464 | |||
| OCUB-M | Growth Inhibition Assay | IC50=25.4456 μM | 21711054 | |||
| MKN45 | Growth Inhibition Assay | IC50=25.6315 μM | 26025875 | |||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=25.7285 μM | 18588281 | |||
| RVH-421 | Growth Inhibition Assay | IC50=25.8161 μM | 20873740 | |||
| NKS-81-FD | Growth Inhibition Assay | IC50=25.9021 μM | 28221790 | |||
| NCI-H596 | Growth Inhibition Assay | IC50=26.0487 μM | 25703296 | |||
| GB-1 | Growth Inhibition Assay | IC50=26.1879 μM | 17602464 | |||
| ZR-75-30 | Growth Inhibition Assay | IC50=26.2297 μM | 17602464 | |||
| U-2-OS | Growth Inhibition Assay | IC50=26.3757 μM | 22342146 | |||
| HuP-T3 | Growth Inhibition Assay | IC50=26.6102 μM | 21711054 | |||
| MOLT-16 | Growth Inhibition Assay | IC50=26.6166 μM | 17602464 | |||
| U-87-MG | Growth Inhibition Assay | IC50=26.7438 μM | 19362474 | |||
| 8505C | Growth Inhibition Assay | IC50=26.9126 μM | 18588281 | |||
| SK-MEL-3 | Growth Inhibition Assay | IC50=26.9828 μM | 22342146 | |||
| COLO-824 | Growth Inhibition Assay | IC50=27.2195 μM | 24631359 | |||
| EW-1 | Growth Inhibition Assay | IC50=27.3554 μM | 29656202 | |||
| UACC-257 | Growth Inhibition Assay | IC50=27.3804 μM | 28221790 | |||
| Hs-578-T | Growth Inhibition Assay | IC50=27.5299 μM | 24631359 | |||
| UACC-893 | Growth Inhibition Assay | IC50=27.6631 μM | 22342146 | |||
| MHH-NB-11 | Growth Inhibition Assay | IC50=27.8007 μM | 20873740 | |||
| KYSE-410 | Growth Inhibition Assay | IC50=28.2779 μM | 21711054 | |||
| SF126 | Growth Inhibition Assay | IC50=28.7435 μM | 21711054 | |||
| HT-144 | Growth Inhibition Assay | IC50=29.3362 μM | 22342146 | |||
| SW1573 | Growth Inhibition Assay | IC50=29.3509 μM | 26025875 | |||
| SW620 | Growth Inhibition Assay | IC50=29.3641 μM | 28075592 | |||
| SCH | Growth Inhibition Assay | IC50=29.8831 μM | 20873740 | |||
| EW-22 | Growth Inhibition Assay | IC50=30.1969 μM | 25703296 | |||
| H4 | Growth Inhibition Assay | IC50=30.4654 μM | 26025875 | |||
| CAS-1 | Growth Inhibition Assay | IC50=30.7859 μM | 24471998 | |||
| MG-63 | Growth Inhibition Assay | IC50=30.8478 μM | 21711054 | |||
| MDA-MB-415 | Growth Inhibition Assay | IC50=31.1753 μM | 18469809 | |||
| NCI-H1395 | Growth Inhibition Assay | IC50=31.2328 μM | 19362474 | |||
| Ca-Ski | Growth Inhibition Assay | IC50=31.3177 μM | 18469809 | |||
| BxPC-3 | Growth Inhibition Assay | IC50=31.3729 μM | 24631359 | |||
| A3-KAW | Growth Inhibition Assay | IC50=31.4471 μM | 17602464 | |||
| T-24 | Growth Inhibition Assay | IC50=31.7362 μM | 20580554 | |||
| NCI-H2029 | Growth Inhibition Assay | IC50=31.7765 μM | 24471998 | |||
| YAPC | Growth Inhibition Assay | IC50=32.0407 μM | 21711054 | |||
| SK-MEL-2 | Growth Inhibition Assay | IC50=32.052 μM | 19362474 | |||
| LS-513 | Growth Inhibition Assay | IC50=32.1187 μM | 19362474 | |||
| AsPC-1 | Growth Inhibition Assay | IC50=32.3605 μM | 17101674 | |||
| KYSE-150 | Growth Inhibition Assay | IC50=32.3773 μM | 23230131 | |||
| NCI-H520 | Growth Inhibition Assay | IC50=32.4482 μM | 21711054 | |||
| JEG-3 | Growth Inhibition Assay | IC50=33.0971 μM | 23230131 | |||
| GMS-10 | Growth Inhibition Assay | IC50=33.3004 μM | 21711054 | |||
| HT-1080 | Growth Inhibition Assay | IC50=33.39 μM | 24195466 | |||
| NCI-H1651 | Growth Inhibition Assay | IC50=33.396 μM | 19362474 | |||
| NCI-H2122 | Growth Inhibition Assay | IC50=33.5574 μM | 20873740 | |||
| ES5 | Growth Inhibition Assay | IC50=33.7292 μM | 29656202 | |||
| 8305C | Growth Inhibition Assay | IC50=33.9937 μM | 19362474 | |||
| KM12 | Growth Inhibition Assay | IC50=34.0478 μM | 23230131 | |||
| HCT-15 | Growth Inhibition Assay | IC50=34.127 μM | 23968824 | |||
| OVCAR-5 | Growth Inhibition Assay | IC50=34.2182 μM | 24867590 | |||
| NCI-H2291 | Growth Inhibition Assay | IC50=34.2472 μM | 23230131 | |||
| CP50-MEL-B | Growth Inhibition Assay | IC50=34.6592 μM | 25105722 | |||
| C-33-A | Growth Inhibition Assay | IC50=34.6857 μM | 27966950 | |||
| NCI-H2452 | Growth Inhibition Assay | IC50=34.7882 μM | 21711054 | |||
| MDA-MB-157 | Growth Inhibition Assay | IC50=34.8193 μM | 19362474 | |||
| LN-405 | Growth Inhibition Assay | IC50=35.4308 μM | 20873740 | |||
| MDA-MB-231 | Growth Inhibition Assay | IC50=35.5054 μM | 23360104 | |||
| EW-24 | Growth Inhibition Assay | IC50=35.6335 μM | 23968824 | |||
| MKN28 | Growth Inhibition Assay | IC50=35.8236 μM | 19362474 | |||
| KINGS-1 | Growth Inhibition Assay | IC50=35.8434 μM | 29328656 | |||
| LC-2-ad | Growth Inhibition Assay | IC50=36.699 μM | 25703296 | |||
| IGR-1 | Growth Inhibition Assay | IC50=36.7075 μM | 24436994 | |||
| SW626 | Growth Inhibition Assay | IC50=37.0417 μM | 22512908 | |||
| ONS-76 | Growth Inhibition Assay | IC50=37.1309 μM | 23968824 | |||
| T98G | Growth Inhibition Assay | IC50=37.8635 μM | 21711054 | |||
| NB14 | Growth Inhibition Assay | IC50=38.4544 μM | 24436994 | |||
| D-423MG | Growth Inhibition Assay | IC50=38.4869 μM | 19362474 | |||
| NCI-H510A | Growth Inhibition Assay | IC50=38.6451 μM | 28495081 | |||
| NMC-G1 | Growth Inhibition Assay | IC50=38.7222 μM | 21711054 | |||
| SW948 | Growth Inhibition Assay | IC50=38.8949 μM | 24341356 | |||
| MFM-223 | Growth Inhibition Assay | IC50=38.9431 μM | 17419604 | |||
| PAN1 | Growth Inhibition Assay | IC50=38.9919 μM | 22512908 | |||
| MZ7-mel | Growth Inhibition Assay | IC50=39.1199 μM | 28075592 | |||
| COLO-679 | Growth Inhibition Assay | IC50=39.9708 μM | 21711054 | |||
| SW872 | Growth Inhibition Assay | IC50=40.2031 μM | 24631359 | |||
| HT-1197 | Growth Inhibition Assay | IC50=40.2869 μM | 27349332 | |||
| ES6 | Growth Inhibition Assay | IC50=40.4552 μM | 18186604 | |||
| SNU-387 | Growth Inhibition Assay | IC50=40.8238 μM | 17419604 | |||
| T47D | Growth Inhibition Assay | IC50=41.0192 μM | 18186604 | |||
| G-402 | Growth Inhibition Assay | IC50=41.0809 μM | 23489626 | |||
| MZ1-PC | Growth Inhibition Assay | IC50=41.81 μM | 17602464 | |||
| SW1417 | Growth Inhibition Assay | IC50=42.303 μM | 17602464 | |||
| RERF-LC-MS | Growth Inhibition Assay | IC50=42.5087 μM | 28576633 | |||
| SF539 | Growth Inhibition Assay | IC50=42.5529 μM | 23489626 | |||
| ESS-1 | Growth Inhibition Assay | IC50=43.5558 μM | 28576633 | |||
| RO82-W-1 | Growth Inhibition Assay | IC50=43.6153 μM | 28576633 | |||
| S-117 | Growth Inhibition Assay | IC50=43.6958 μM | 22512908 | |||
| SW756 | Growth Inhibition Assay | IC50=43.8242 μM | SANGER | |||
| CP66-MEL | Growth Inhibition Assay | IC50=45.7143 μM | SANGER | |||
| H-EMC-SS | Growth Inhibition Assay | IC50=45.7693 μM | SANGER | |||
| NCI-H2052 | Growth Inhibition Assay | IC50=45.9027 μM | SANGER | |||
| SW684 | Growth Inhibition Assay | IC50=47.0081 μM | SANGER | |||
| HCC1569 | Growth Inhibition Assay | IC50=47.1658 μM | SANGER | |||
| KGN | Growth Inhibition Assay | IC50=47.3311 μM | SANGER | |||
| LCLC-103H | Growth Inhibition Assay | IC50=47.4404 μM | SANGER | |||
| SW780 | Growth Inhibition Assay | IC50=47.6351 μM | SANGER | |||
| NCI-H1703 | Growth Inhibition Assay | IC50=48.3352 μM | SANGER | |||
| HCC1395 | Growth Inhibition Assay | IC50=48.7432 μM | SANGER | |||
| Click to View More Cell Line Experimental Data | ||||||
Biological Activity
| Description | Gefitinib is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway. | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Features | A potent EGFR tyrosine kinase inhibitor. | ||||||||
| Targets |
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| In vitro | ||||
| In vitro | Gefitinib effectively inhibits all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines including NR6, NR6M and NR6W cell lines. The phosphorylation sites Tyr1173 and Tyr992 are less sensitive requiring higher concentrations of Gefitinib for inhibition. Gefitinib effectively blocks the phosphorylation of PLC-γ, with IC50 of 27nM, in NR6W cells. The NR6wtEGFR and NR6M cell lines has low levels of PLC-γ phosphorylation but the level in the NR6M cell line is more resistant to inhibition by Gefitinib with IC50 of 43 nM and 369 nM, respectively. Gefitinib inhibits Akt phosphorylations, with IC50 of 220 and 263nM, in the low-EGFR- and -EGFRvIII-expressing cell lines, respectively. Gefitinib in the dose range from 0.1 to 0.5μM significantly facilitates, rather than abrogates, colony formation of NR6M cells. However, at a concentration of 2 μM Gefitinib completely blocks NR6M colony formation. Gefitinib rapidly and in a dose-dependent manner inhibits EGFR and ERK phosphorylation up to 72 hours after EGF stimulation in both the high- and low-EGFR-expressing cell lines. [1] Gefitinib is the monolayer growth of these EGF-driven untransformed MCF10A cells with an IC50 of 20 nM. [2] The combination of Gefitinib (0.2 μM and 0.5 μM) with irradiation lead to a significant growth inhibition in LoVo cells, compared with radiation alone.. [3] |
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|---|---|---|---|---|
| Cell Research | Cell lines | NR6, NR6M and NR6W cells | ||
| Concentrations | 0-2 μM | |||
| Incubation Time | 72 hours | |||
| Method | Exponentially growing cells including NR6, NR6M, NR6M and NR6W cells are seeded in sextuple in 96-well plates at a concentration of 2000 cells/well, allowed to adhere and subsequently washed in PBS and incubated overnight in medium containing 0.5% FCS. Cells are then treated with varying concentrations (0-2 μM) of Gefitinib or the solute control DMSO and EGF. The optimal EGF concentration for inducing proliferation of NR6wtEGFR and NR6W cells has previously been determined and hence NR6wtEGFR and NR6W cells are supplemented with 10 nM and 0.1 nM EGF, respectively. EGF is not added to NR6 and NR6M cells. After 72 hours the amount of cells are measured by performing a MTT proliferation assay. |
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| Experimental Result Images | Methods | Biomarkers | Images | PMID |
| Western blot | phospho-EGFR / phospho-ERK / phospho-SRC / phospho-AKT Cyclin D1/ p16 / p27 / pRb uc-caspase-9 / c-caspase-9 / uc-caspase-3 / c-caspase-3 / uc-PARP / PARP PPAR-γ |
|
22586683 | |
| Immunofluorescence | EGFR / LC3 PPAR-γ p-EGFR / β-catenin |
|
31196210 | |
| Growth inhibition assay | GI50 |
|
23409107 | |
| In Vivo | ||
| In vivo |
Gefitinib (100 mg/kg) improves the anti-tumor effect of radiotherapy in LoVo tumor xenografts. [3] Gefitinib treatment of nude mice bearing established human GEO colon cancer xenografts reveals a reversible dose-dependent inhibition of tumor growth because GEO tumors resumes the growth rate of controls at the end of the treatment. [4] |
|
|---|---|---|
| Animal Research | Animal Models | Female nude mice (cba nu/nu) aged 8–10 weeks are intra-dermal injected with LoVo cells. |
| Dosages | 100 mg/kg | |
| Administration | Once daily by oral administration (0.1 mL/10 g body weight) for 14 days | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03599518 | Terminated | Non Small Cell Lung Cancer | Daiichi Sankyo Co. Ltd.|Daiichi Sankyo Inc. | September 21 2018 | Phase 1 |
| NCT03292133 | Active not recruiting | Lung Cancer | Massachusetts General Hospital|Novartis | October 31 2017 | Phase 2 |
| NCT03122717 | Active not recruiting | Non-Small Cell Lung Cancer | Dana-Farber Cancer Institute|AstraZeneca | May 9 2017 | Phase 1|Phase 2 |
| NCT02932345 | Terminated | EGFR Mutation Positive Advanced Non-small-cell Lung Cancer | AstraZeneca | October 31 2016 | -- |
| NCT02824458 | Unknown status | EGFR Tyrosine Kinase Inhibitors Plus VEGFR Inhibitors | Sun Yat-sen University | June 2016 | Phase 3 |
Chemical lnformation & Solubility
| Molecular Weight | 446.90 | Formula | C22H24ClFN4O3 |
| CAS No. | 184475-35-2 | SDF | Download Gefitinib SDF |
| Smiles | COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4 | ||
| Storage (From the date of receipt) | |||
|
In vitro |
DMSO : 89 mg/mL ( (199.14 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.) Ethanol : 4 mg/mL Water : Insoluble |
Molecular Weight Calculator |
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In vivo Add solvents to the product individually and in order. |
In vivo Formulation Calculator |
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Preparing Stock Solutions
Molarity Calculator
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
Question 1:
I try to dissolve Gefitinib (ZD1839) in 0.5% methylcellulose+0.2% Tween 80 for in vivo experiments. However, when I prepare the mixture, it forms precipitates. Exists another way to dissolve completely the compound?
Answer:
S1025 can be dissovled in both 5% DMSO+corn oil and 5% DMSO+30% PEG 300+5% Tween 80+ddH2O at 2.5 mg/ml clearly. It dissolves in DMSO not readily, please sonicate and warm it in water bath at about 45 degree, and dissolve it clearly first. Then add other solvent.
EGFR Signaling Pathway Map
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