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PF-4708671
PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. PF-4708671 induces autophagy. First S6K1-specific inhibitor to be reported.
PF-4708671 Chemical Structure
CAS: 1255517-76-0
Selleck's PF-4708671 has been cited by 53 publications
Purity & Quality Control
Batch:
Purity:
99.97%
99.97
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Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| BHT-101 | Growth Inhibition Assay | IC50=0.82024 μM | SANGER | |||
| UACC-893 | Growth Inhibition Assay | IC50=5.19886 μM | SANGER | |||
| A427 | Growth Inhibition Assay | IC50=5.72567 μM | SANGER | |||
| OCUB-M | Growth Inhibition Assay | IC50=6.66102 μM | SANGER | |||
| SW684 | Growth Inhibition Assay | IC50=7.52268 μM | SANGER | |||
| SK-LMS-1 | Growth Inhibition Assay | IC50=9.01302 μM | SANGER | |||
| CP50-MEL-B | Growth Inhibition Assay | IC50=9.30419 μM | SANGER | |||
| NCI-H1651 | Growth Inhibition Assay | IC50=10.0276 μM | SANGER | |||
| ABC-1 | Growth Inhibition Assay | IC50=10.1037 μM | SANGER | |||
| OE19 | Growth Inhibition Assay | IC50=10.1733 μM | SANGER | |||
| DSH1 | Growth Inhibition Assay | IC50=10.8879 μM | SANGER | |||
| SW13 | Growth Inhibition Assay | IC50=11.9319 μM | SANGER | |||
| MDA-MB-453 | Growth Inhibition Assay | IC50=12.1603 μM | SANGER | |||
| 647-V | Growth Inhibition Assay | IC50=12.3582 μM | SANGER | |||
| NCI-H2342 | Growth Inhibition Assay | IC50=12.3995 μM | SANGER | |||
| LB2241-RCC | Growth Inhibition Assay | IC50=12.5779 μM | SANGER | |||
| UACC-257 | Growth Inhibition Assay | IC50=13.4453 μM | SANGER | |||
| NCI-H661 | Growth Inhibition Assay | IC50=13.6449 μM | SANGER | |||
| FADU | Growth Inhibition Assay | IC50=13.6992 μM | SANGER | |||
| A2780 | Growth Inhibition Assay | IC50=13.8041 μM | SANGER | |||
| NCI-H1793 | Growth Inhibition Assay | IC50=14.4085 μM | SANGER | |||
| TE-8 | Growth Inhibition Assay | IC50=15.3465 μM | SANGER | |||
| HGC-27 | Growth Inhibition Assay | IC50=16.1644 μM | SANGER | |||
| MMAC-SF | Growth Inhibition Assay | IC50=17.3727 μM | SANGER | |||
| Calu-6 | Growth Inhibition Assay | IC50=18.1513 μM | SANGER | |||
| HUTU-80 | Growth Inhibition Assay | IC50=18.3959 μM | SANGER | |||
| SAS | Growth Inhibition Assay | IC50=18.6455 μM | SANGER | |||
| IST-MES1 | Growth Inhibition Assay | IC50=18.6508 μM | SANGER | |||
| C3A | Growth Inhibition Assay | IC50=18.7919 μM | SANGER | |||
| ES3 | Growth Inhibition Assay | IC50=18.8364 μM | SANGER | |||
| HSC-2 | Growth Inhibition Assay | IC50=19.6541 μM | SANGER | |||
| T47D | Growth Inhibition Assay | IC50=20.1485 μM | SANGER | |||
| EW-7 | Growth Inhibition Assay | IC50=20.8588 μM | SANGER | |||
| LN-405 | Growth Inhibition Assay | IC50=20.8965 μM | SANGER | |||
| U031 | Growth Inhibition Assay | IC50=21.4802 μM | SANGER | |||
| A549 | Growth Inhibition Assay | IC50=21.8491 μM | SANGER | |||
| RMG-I | Growth Inhibition Assay | IC50=22.2668 μM | SANGER | |||
| BT-474 | Growth Inhibition Assay | IC50=22.6551 μM | SANGER | |||
| NB69 | Growth Inhibition Assay | IC50=23.152 μM | SANGER | |||
| NB7 | Growth Inhibition Assay | IC50=24.188 μM | SANGER | |||
| HCC1569 | Growth Inhibition Assay | IC50=24.6125 μM | SANGER | |||
| MEL-JUSO | Growth Inhibition Assay | IC50=24.6908 μM | SANGER | |||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=25.2517 μM | SANGER | |||
| HCC1419 | Growth Inhibition Assay | IC50=25.6003 μM | SANGER | |||
| Ca9-22 | Growth Inhibition Assay | IC50=25.6432 μM | SANGER | |||
| KGN | Growth Inhibition Assay | IC50=25.7547 μM | SANGER | |||
| LB373-MEL-D | Growth Inhibition Assay | IC50=26.1938 μM | SANGER | |||
| NCI-H1755 | Growth Inhibition Assay | IC50=26.8841 μM | SANGER | |||
| D-423MG | Growth Inhibition Assay | IC50=27.0715 μM | SANGER | |||
| DK-MG | Growth Inhibition Assay | IC50=28.7846 μM | SANGER | |||
| NCI-H1623 | Growth Inhibition Assay | IC50=28.8342 μM | SANGER | |||
| KU-19-19 | Growth Inhibition Assay | IC50=28.995 μM | SANGER | |||
| C-33-A | Growth Inhibition Assay | IC50=29.2198 μM | SANGER | |||
| SCC-4 | Growth Inhibition Assay | IC50=30.3354 μM | SANGER | |||
| MG-63 | Growth Inhibition Assay | IC50=30.5994 μM | SANGER | |||
| LNCaP-Clone-FGC | Growth Inhibition Assay | IC50=31.4921 μM | SANGER | |||
| CAPAN-1 | Growth Inhibition Assay | IC50=31.5286 μM | SANGER | |||
| GI-ME-N | Growth Inhibition Assay | IC50=31.5353 μM | SANGER | |||
| RERF-LC-MS | Growth Inhibition Assay | IC50=32.6747 μM | SANGER | |||
| KLE | Growth Inhibition Assay | IC50=33.4334 μM | SANGER | |||
| KNS-81-FD | Growth Inhibition Assay | IC50=33.5008 μM | SANGER | |||
| DOK | Growth Inhibition Assay | IC50=34.6612 μM | SANGER | |||
| ACHN | Growth Inhibition Assay | IC50=35.1588 μM | SANGER | |||
| KYSE-520 | Growth Inhibition Assay | IC50=35.2361 μM | SANGER | |||
| SBC-5 | Growth Inhibition Assay | IC50=35.5116 μM | SANGER | |||
| NCI-H28 | Growth Inhibition Assay | IC50=35.6695 μM | SANGER | |||
| ES7 | Growth Inhibition Assay | IC50=36.2249 μM | SANGER | |||
| A172 | Growth Inhibition Assay | IC50=36.4187 μM | SANGER | |||
| UM-UC-3 | Growth Inhibition Assay | IC50=37.8746 μM | SANGER | |||
| LXF-289 | Growth Inhibition Assay | IC50=38.0047 μM | SANGER | |||
| KP-4 | Growth Inhibition Assay | IC50=38.4739 μM | SANGER | |||
| TE-1 | Growth Inhibition Assay | IC50=39.6589 μM | SANGER | |||
| G-402 | Growth Inhibition Assay | IC50=40.061 μM | SANGER | |||
| 786-0 | Growth Inhibition Assay | IC50=40.9096 μM | SANGER | |||
| K5 | Growth Inhibition Assay | IC50=41.3686 μM | SANGER | |||
| SK-N-DZ | Growth Inhibition Assay | IC50=41.3823 μM | SANGER | |||
| OVCAR-4 | Growth Inhibition Assay | IC50=41.7568 μM | SANGER | |||
| T84 | Growth Inhibition Assay | IC50=42.1263 μM | SANGER | |||
| GCIY | Growth Inhibition Assay | IC50=43.0803 μM | SANGER | |||
| BB49-HNC | Growth Inhibition Assay | IC50=43.3348 μM | SANGER | |||
| SNU-C2B | Growth Inhibition Assay | IC50=43.6436 μM | SANGER | |||
| TE-6 | Growth Inhibition Assay | IC50=43.8894 μM | SANGER | |||
| 23132-87 | Growth Inhibition Assay | IC50=44.2978 μM | SANGER | |||
| DMS-53 | Growth Inhibition Assay | IC50=44.3384 μM | SANGER | |||
| ONS-76 | Growth Inhibition Assay | IC50=44.7661 μM | SANGER | |||
| DMS-273 | Growth Inhibition Assay | IC50=44.943 μM | SANGER | |||
| COLO-824 | Growth Inhibition Assay | IC50=45.8775 μM | SANGER | |||
| DMS-114 | Growth Inhibition Assay | IC50=45.8927 μM | SANGER | |||
| YKG-1 | Growth Inhibition Assay | IC50=46.0355 μM | SANGER | |||
| RH-18 | Growth Inhibition Assay | IC50=46.3733 μM | SANGER | |||
| NCI-H1355 | Growth Inhibition Assay | IC50=46.618 μM | SANGER | |||
| NCI-H2170 | Growth Inhibition Assay | IC50=47.7584 μM | SANGER | |||
| OC-314 | Growth Inhibition Assay | IC50=47.8478 μM | SANGER | |||
| NCI-H2030 | Growth Inhibition Assay | IC50=47.8906 μM | SANGER | |||
| 22RV1 | Growth Inhibition Assay | IC50=47.9015 μM | SANGER | |||
| G-401 | Growth Inhibition Assay | IC50=48.4415 μM | SANGER | |||
| YAPC | Growth Inhibition Assay | IC50=49.8073 μM | SANGER | |||
| SW1573 | Growth Inhibition Assay | IC50=50.2435 μM | SANGER | |||
| COLO-792 | Growth Inhibition Assay | IC50=50.6237 μM | SANGER | |||
| KNS-62 | Growth Inhibition Assay | IC50=50.7508 μM | SANGER | |||
| NB5 | Growth Inhibition Assay | IC50=51.4509 μM | SANGER | |||
| CP66-MEL | Growth Inhibition Assay | IC50=51.6408 μM | SANGER | |||
| CaR-1 | Growth Inhibition Assay | IC50=52.0606 μM | SANGER | |||
| CAL-54 | Growth Inhibition Assay | IC50=52.1102 μM | SANGER | |||
| 8305C | Growth Inhibition Assay | IC50=52.315 μM | SANGER | |||
| Calu-3 | Growth Inhibition Assay | IC50=52.3733 μM | SANGER | |||
| AU565 | Growth Inhibition Assay | IC50=52.5509 μM | SANGER | |||
| CW-2 | Growth Inhibition Assay | IC50=52.8654 μM | SANGER | |||
| BEN | Growth Inhibition Assay | IC50=53.7862 μM | SANGER | |||
| NCI-H1975 | Growth Inhibition Assay | IC50=53.8966 μM | SANGER | |||
| HCT-116 | Growth Inhibition Assay | IC50=54.0327 μM | SANGER | |||
| SH-4 | Growth Inhibition Assay | IC50=54.138 μM | SANGER | |||
| NCI-H1693 | Growth Inhibition Assay | IC50=54.2103 μM | SANGER | |||
| BPH-1 | Growth Inhibition Assay | IC50=55.2892 μM | SANGER | |||
| CAMA-1 | Growth Inhibition Assay | IC50=55.8116 μM | SANGER | |||
| A388 | Growth Inhibition Assay | IC50=56.0985 μM | SANGER | |||
| C2BBe1 | Growth Inhibition Assay | IC50=56.2634 μM | SANGER | |||
| GAMG | Growth Inhibition Assay | IC50=56.5955 μM | SANGER | |||
| MKN28 | Growth Inhibition Assay | IC50=56.8013 μM | SANGER | |||
| VA-ES-BJ | Growth Inhibition Assay | IC50=56.8745 μM | SANGER | |||
| HuCCT1 | Growth Inhibition Assay | IC50=57.0492 μM | SANGER | |||
| BFTC-905 | Growth Inhibition Assay | IC50=57.2898 μM | SANGER | |||
| LS-123 | Growth Inhibition Assay | IC50=57.5668 μM | SANGER | |||
| LB996-RCC | Growth Inhibition Assay | IC50=58.0287 μM | SANGER | |||
| NCI-H1048 | Growth Inhibition Assay | IC50=58.2188 μM | SANGER | |||
| COR-L105 | Growth Inhibition Assay | IC50=58.7337 μM | SANGER | |||
| OVCAR-8 | Growth Inhibition Assay | IC50=59.1716 μM | SANGER | |||
| SK-N-FI | Growth Inhibition Assay | IC50=59.3207 μM | SANGER | |||
| MES-SA | Growth Inhibition Assay | IC50=59.4509 μM | SANGER | |||
| SCC-9 | Growth Inhibition Assay | IC50=59.4753 μM | SANGER | |||
| EFO-27 | Growth Inhibition Assay | IC50=59.943 μM | SANGER | |||
| GT3TKB | Growth Inhibition Assay | IC50=60.6048 μM | SANGER | |||
| HCC38 | Growth Inhibition Assay | IC50=61.4379 μM | SANGER | |||
| MLMA | Growth Inhibition Assay | IC50=61.6163 μM | SANGER | |||
| D-566MG | Growth Inhibition Assay | IC50=63.5224 μM | SANGER | |||
| SF295 | Growth Inhibition Assay | IC50=63.6655 μM | SANGER | |||
| ES4 | Growth Inhibition Assay | IC50=64.4719 μM | SANGER | |||
| CAKI-1 | Growth Inhibition Assay | IC50=64.5721 μM | SANGER | |||
| OAW-28 | Growth Inhibition Assay | IC50=64.9647 μM | SANGER | |||
| NCI-H460 | Growth Inhibition Assay | IC50=65.0897 μM | SANGER | |||
| JAR | Growth Inhibition Assay | IC50=65.5516 μM | SANGER | |||
| SNU-449 | Growth Inhibition Assay | IC50=65.7616 μM | SANGER | |||
| D-392MG | Growth Inhibition Assay | IC50=65.9434 μM | SANGER | |||
| EW-22 | Growth Inhibition Assay | IC50=66.395 μM | SANGER | |||
| GCT | Growth Inhibition Assay | IC50=67.0443 μM | SANGER | |||
| NOS-1 | Growth Inhibition Assay | IC50=67.6867 μM | SANGER | |||
| RH-1 | Growth Inhibition Assay | IC50=68.5559 μM | SANGER | |||
| HuH-7 | Growth Inhibition Assay | IC50=69.1002 μM | SANGER | |||
| NUGC-3 | Growth Inhibition Assay | IC50=70.9644 μM | SANGER | |||
| IST-SL1 | Growth Inhibition Assay | IC50=71.2324 μM | SANGER | |||
| SHP-77 | Growth Inhibition Assay | IC50=72.119 μM | SANGER | |||
| SW1116 | Growth Inhibition Assay | IC50=72.1407 μM | SANGER | |||
| LK-2 | Growth Inhibition Assay | IC50=72.8612 μM | SANGER | |||
| U-2-OS | Growth Inhibition Assay | IC50=73.1828 μM | SANGER | |||
| KYSE-150 | Growth Inhibition Assay | IC50=73.6118 μM | SANGER | |||
| U251 | Growth Inhibition Assay | IC50=73.8168 μM | SANGER | |||
| HT-1080 | Growth Inhibition Assay | IC50=74.2574 μM | SANGER | |||
| NCI-H1437 | Growth Inhibition Assay | IC50=74.6326 μM | SANGER | |||
| HPAF-II | Growth Inhibition Assay | IC50=74.6415 μM | SANGER | |||
| Becker | Growth Inhibition Assay | IC50=75.1105 μM | SANGER | |||
| PANC-10-05 | Growth Inhibition Assay | IC50=75.2865 μM | SANGER | |||
| TYK-nu | Growth Inhibition Assay | IC50=75.3102 μM | SANGER | |||
| SKG-IIIa | Growth Inhibition Assay | IC50=75.3341 μM | SANGER | |||
| NCI-H1993 | Growth Inhibition Assay | IC50=75.7397 μM | SANGER | |||
| S-117 | Growth Inhibition Assay | IC50=75.755 μM | SANGER | |||
| HuO9 | Growth Inhibition Assay | IC50=76.0048 μM | SANGER | |||
| CAL-51 | Growth Inhibition Assay | IC50=76.1006 μM | SANGER | |||
| BT-20 | Growth Inhibition Assay | IC50=76.2168 μM | SANGER | |||
| LB831-BLC | Growth Inhibition Assay | IC50=76.3217 μM | SANGER | |||
| LB1047-RCC | Growth Inhibition Assay | IC50=76.7619 μM | SANGER | |||
| ES8 | Growth Inhibition Assay | IC50=78.0073 μM | SANGER | |||
| UMC-11 | Growth Inhibition Assay | IC50=78.0884 μM | SANGER | |||
| NCI-H226 | Growth Inhibition Assay | IC50=78.1315 μM | SANGER | |||
| IGROV-1 | Growth Inhibition Assay | IC50=78.555 μM | SANGER | |||
| BHY | Growth Inhibition Assay | IC50=79.596 μM | SANGER | |||
| MKN45 | Growth Inhibition Assay | IC50=80.3174 μM | SANGER | |||
| IA-LM | Growth Inhibition Assay | IC50=80.3511 μM | SANGER | |||
| WM-115 | Growth Inhibition Assay | IC50=81.4114 μM | SANGER | |||
| VMRC-RCZ | Growth Inhibition Assay | IC50=81.4425 μM | SANGER | |||
| NCI-H2291 | Growth Inhibition Assay | IC50=81.6842 μM | SANGER | |||
| MCF7 | Growth Inhibition Assay | IC50=83.2897 μM | SANGER | |||
| 639-V | Growth Inhibition Assay | IC50=84.6129 μM | SANGER | |||
| RT4 | Growth Inhibition Assay | IC50=85.2403 μM | SANGER | |||
| NCI-H2405 | Growth Inhibition Assay | IC50=85.2997 μM | SANGER | |||
| CAL-33 | Growth Inhibition Assay | IC50=85.6315 μM | SANGER | |||
| BT-549 | Growth Inhibition Assay | IC50=85.9382 μM | SANGER | |||
| HT-1197 | Growth Inhibition Assay | IC50=88.1077 μM | SANGER | |||
| G-361 | Growth Inhibition Assay | IC50=88.1474 μM | SANGER | |||
| LS-411N | Growth Inhibition Assay | IC50=89.3388 μM | SANGER | |||
| HT-144 | Growth Inhibition Assay | IC50=89.5992 μM | SANGER | |||
| DJM-1 | Growth Inhibition Assay | IC50=89.8845 μM | SANGER | |||
| CAL-12T | Growth Inhibition Assay | IC50=90.7895 μM | SANGER | |||
| MKN7 | Growth Inhibition Assay | IC50=91.3551 μM | SANGER | |||
| HuP-T3 | Growth Inhibition Assay | IC50=96.1004 μM | SANGER | |||
| SK-MG-1 | Growth Inhibition Assay | IC50=96.1348 μM | SANGER | |||
| NCI-H2347 | Growth Inhibition Assay | IC50=98.1042 μM | SANGER | |||
| SW872 | Growth Inhibition Assay | IC50=100.456 μM | SANGER | |||
| COLO-829 | Growth Inhibition Assay | IC50=100.553 μM | SANGER | |||
| MC-IXC | Growth Inhibition Assay | IC50=100.615 μM | SANGER | |||
| Click to View More Cell Line Experimental Data | ||||||
Biological Activity
| Description | PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. PF-4708671 induces autophagy. First S6K1-specific inhibitor to be reported. | ||
|---|---|---|---|
| Targets |
|
| In vitro | ||||
| In vitro | PF-4708671 is a piperazinyl-pyrimidine analogue and the first S6K1-specific inhibitor. PF-4708671 does not significantly inhibit the activity of the closely related S6K2 isoform or a number of other AGC kinases (Akt1, Akt2, PKA, PKCα, PKCϵ, PRK2, ROCK2, RSK1, RSK2 or SGK1) . PF-4708671 prevents the S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1), while having no effect upon the PMA-induced phosphorylation of substrates of the highly related RSK (p90 ribosomal S6 kinase) and MSK (mitogen- and stress-activated kinase) kinases. PF-4708671 is also found to induce phosphorylation of the T-loop and hydrophobic motif of S6K1, an effect that is dependent upon mTORC1 (mTOR complex 1). PF-4708671 does not affect activity of mTORC1. [1] | |||
|---|---|---|---|---|
| Experimental Result Images | Methods | Biomarkers | Images | PMID |
| Western blot | pS6 / S6 / pS6K / S6K1 / pAKT / AKT p-mTOR / mTOR / p-p70S6K / p70S6K |
|
28626016 | |
| Growth inhibition assay | Cell viability |
|
30423811 | |
Chemical lnformation & Solubility
| Molecular Weight | 390.41 | Formula | C19H21F3N6 |
| CAS No. | 1255517-76-0 | SDF | Download PF-4708671 SDF |
| Smiles | CCC1=CN=CN=C1N2CCN(CC2)CC3=NC4=C(N3)C=C(C=C4)C(F)(F)F | ||
| Storage (From the date of receipt) | |||
|
In vitro |
DMSO : 30 mg/mL ( (76.84 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.) Ethanol : 8 mg/mL Water : Insoluble |
Molecular Weight Calculator |
|
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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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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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.
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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:
Whether the in vivo formula "30% PEG400+0.5% Tween80+5% Propylene glycol" for S2163 is suitable for i.p. or not?
Answer:
The formula "30% PEG400+0.5% Tween80+5% Propylene glycol" on our website is an oral one. It is a suspension.
S6 Kinase Signaling Pathway Map
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