Home PI3K/Akt/mTOR Akt inhibitor - Autophagy activator - Apoptosis related activator MK-2206 2HCl For research use only.

MK-2206 2HCl

MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.

MK-2206 2HCl Chemical Structure

MK-2206 2HCl Chemical Structure

CAS: 1032350-13-2

Selleck's MK-2206 2HCl has been cited by 1816 publications

Purity & Quality Control

Batch: Purity: 99.98%
99.98

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NCI-H69 Growth Inhibition Assay IC50=441.083 μM SANGER
HCC38 Growth Inhibition Assay IC50=401.593 μM SANGER
NCI-H2052 Growth Inhibition Assay IC50=398.472 μM SANGER
NB17 Growth Inhibition Assay IC50=392.596 μM SANGER
SBC-5 Growth Inhibition Assay IC50=386.985 μM SANGER
K-562 Growth Inhibition Assay IC50=383.36 μM SANGER
T84 Growth Inhibition Assay IC50=374.712 μM SANGER
LU-135 Growth Inhibition Assay IC50=367.035 μM SANGER
TE-9 Growth Inhibition Assay IC50=363.589 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=347.401 μM SANGER
BE-13 Growth Inhibition Assay IC50=344.167 μM SANGER
NCI-H1993 Growth Inhibition Assay IC50=342.365 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=342.326 μM SANGER
NCI-H630 Growth Inhibition Assay IC50=332.294 μM SANGER
KP-N-YN Growth Inhibition Assay IC50=341.123 μM SANGER
C3A Growth Inhibition Assay IC50=311.802 μM SANGER
HEL Growth Inhibition Assay IC50=309.983 μM SANGER
NCI-H810 Growth Inhibition Assay IC50=310.57 μM SANGER
LU-65 Growth Inhibition Assay IC50=304.32 μM SANGER
L-428 Growth Inhibition Assay IC50=297.616 μM SANGER
FADU Growth Inhibition Assay IC50=297.51 μM SANGER
IGR-1 Growth Inhibition Assay IC50=295.659 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=294.409 μM SANGER
C8166 Growth Inhibition Assay IC50=278.506 μM SANGER
TGBC11TKB Growth Inhibition Assay IC50=278.178 μM SANGER
RERF-LC-MS Growth Inhibition Assay IC50=276.007 μM SANGER
COLO-680N Growth Inhibition Assay IC50=272.527 μM SANGER
NB6 Growth Inhibition Assay IC50=270.1 μM SANGER
GAK Growth Inhibition Assay IC50=253.002 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=249.27 μM SANGER
NCI-H2347 Growth Inhibition Assay IC50=247.713 μM SANGER
LS-1034 Growth Inhibition Assay IC50=246.266 μM SANGER
SH-4 Growth Inhibition Assay IC50=246.09 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=243.795 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=231.905 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=216.125 μM SANGER
KNS-42 Growth Inhibition Assay IC50=216.574 μM SANGER
RCM-1 Growth Inhibition Assay IC50=214.762 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=207.909 μM SANGER
SW982 Growth Inhibition Assay IC50=207.948 μM SANGER
SW1116 Growth Inhibition Assay IC50=207.077 μM SANGER
HuCCT1 Growth Inhibition Assay IC50=204.208 μM SANGER
NCI-H650 Growth Inhibition Assay IC50=202.103 μM SANGER
COLO-678 Growth Inhibition Assay IC50=201.45 μM SANGER
HT-29 Growth Inhibition Assay IC50=201.212 μM SANGER
SCC-9 Growth Inhibition Assay IC50=191 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=191.888 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=188.333 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=186.84 μM SANGER
CAL-72 Growth Inhibition Assay IC50=185.054 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=180.165 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=178.467 μM SANGER
no-10 Growth Inhibition Assay IC50=178.134 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=177.503 μM SANGER
HCE-4 Growth Inhibition Assay IC50=166.845 μM SANGER
NY Growth Inhibition Assay IC50=165.314 μM SANGER
A673 Growth Inhibition Assay IC50=161.705 μM SANGER
SAS Growth Inhibition Assay IC50=162.678 μM SANGER
Capan-2 Growth Inhibition Assay IC50=160.553 μM SANGER
KU812 Growth Inhibition Assay IC50=158.674 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=154.694 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=153.064 μM SANGER
BEN Growth Inhibition Assay IC50=153.928 μM SANGER
KYSE-450 Growth Inhibition Assay IC50=151.539 μM SANGER
GT3TKB Growth Inhibition Assay IC50=149.928 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=147.878 μM SANGER
OVCAR-8 Growth Inhibition Assay IC50=145.636 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=144.501 μM SANGER
COR-L88 Growth Inhibition Assay IC50=142.14 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=139.833 μM SANGER
HCT-116 Growth Inhibition Assay IC50=137.217 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=135.993 μM SANGER
U-87-MG Growth Inhibition Assay IC50=133.604 μM SANGER
NCI-H2087 Growth Inhibition Assay IC50=131.483 μM SANGER
NCI-H1651 Growth Inhibition Assay IC50=131.243 μM SANGER
A2780 Growth Inhibition Assay IC50=128.988 μM SANGER
BALL-1 Growth Inhibition Assay IC50=126.23 μM SANGER
COLO-679 Growth Inhibition Assay IC50=126.753 μM SANGER
SF268 Growth Inhibition Assay IC50=126.158 μM SANGER
SN12C Growth Inhibition Assay IC50=124.176 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=125.514 μM SANGER
NCI-H2452 Growth Inhibition Assay IC50=122.21 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=123.244 μM SANGER
ML-2 Growth Inhibition Assay IC50=121.676 μM SANGER
SW1990 Growth Inhibition Assay IC50=120.951 μM SANGER
D-392MG Growth Inhibition Assay IC50=117.398 μM SANGER
NCI-H1793 Growth Inhibition Assay IC50=109.28 μM SANGER
GOTO Growth Inhibition Assay IC50=107.777 μM SANGER
HLE Growth Inhibition Assay IC50=105.282 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=100.121 μM SANGER
SW684 Growth Inhibition Assay IC50=98.6654 μM SANGER
NCI-H2029 Growth Inhibition Assay IC50=96.9566 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=96.8992 μM SANGER
SCH Growth Inhibition Assay IC50=96.3877 μM SANGER
COLO-792 Growth Inhibition Assay IC50=95.2564 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=92.9106 μM SANGER
TE-10 Growth Inhibition Assay IC50=91.5611 μM SANGER
KYSE-410 Growth Inhibition Assay IC50=91.4042 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=89.9028 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=86.8872 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=86.1977 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=85.4641 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=84.2185 μM SANGER
KY821 Growth Inhibition Assay IC50=84.0892 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=83.4702 μM SANGER
HSC-3 Growth Inhibition Assay IC50=83.3071 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=81.1768 μM SANGER
A3-KAW Growth Inhibition Assay IC50=80.2154 μM SANGER
CAL-62 Growth Inhibition Assay IC50=80.095 μM SANGER
JAR Growth Inhibition Assay IC50=79.0546 μM SANGER
KYSE-180 Growth Inhibition Assay IC50=77.5454 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=77.4243 μM SANGER
MC116 Growth Inhibition Assay IC50=75.5708 μM SANGER
U-266 Growth Inhibition Assay IC50=75.4516 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=74.4048 μM SANGER
NCI-H522 Growth Inhibition Assay IC50=72.3413 μM SANGER
COLO-668 Growth Inhibition Assay IC50=71.8451 μM SANGER
Mewo Growth Inhibition Assay IC50=71.505 μM SANGER
KYSE-70 Growth Inhibition Assay IC50=70.7835 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=70.6705 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=69.9486 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=68.3238 μM SANGER
SW620 Growth Inhibition Assay IC50=66.2039 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=65.8481 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=65.5649 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=65.0095 μM SANGER
KGN Growth Inhibition Assay IC50=64.5514 μM SANGER
BHY Growth Inhibition Assay IC50=64.1245 μM SANGER
C-33-A Growth Inhibition Assay IC50=64.0957 μM SANGER
NCI-H596 Growth Inhibition Assay IC50=62.7496 μM SANGER
LS-411N Growth Inhibition Assay IC50=61.3903 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=60.5294 μM SANGER
647-V Growth Inhibition Assay IC50=60.1347 μM SANGER
COLO-824 Growth Inhibition Assay IC50=60.0719 μM SANGER
TCCSUP Growth Inhibition Assay IC50=59.5279 μM SANGER
JVM-2 Growth Inhibition Assay IC50=58.9506 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=58.4814 μM SANGER
FTC-133 Growth Inhibition Assay IC50=58.0969 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=57.778 μM SANGER
HPAF-II Growth Inhibition Assay IC50=56.4073 μM SANGER
MKN7 Growth Inhibition Assay IC50=56.0285 μM SANGER
UACC-62 Growth Inhibition Assay IC50=55.1046 μM SANGER
IA-LM Growth Inhibition Assay IC50=54.6322 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=49.4793 μM SANGER
HT55 Growth Inhibition Assay IC50=49.1474 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=48.4016 μM SANGER
U-118-MG Growth Inhibition Assay IC50=48.3702 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=48.2845 μM SANGER
SW1573 Growth Inhibition Assay IC50=47.3736 μM SANGER
RO82-W-1 Growth Inhibition Assay IC50=46.9822 μM SANGER
KM12 Growth Inhibition Assay IC50=45.9076 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=45.8967 μM SANGER
TE-11 Growth Inhibition Assay IC50=45.4842 μM SANGER
PSN1 Growth Inhibition Assay IC50=45.2548 μM SANGER
SK-N-AS Growth Inhibition Assay IC50=43.6019 μM SANGER
NCI-H1573 Growth Inhibition Assay IC50=43.3477 μM SANGER
Calu-6 Growth Inhibition Assay IC50=43.2382 μM SANGER
HCC1937 Growth Inhibition Assay IC50=42.7843 μM SANGER
UMC-11 Growth Inhibition Assay IC50=41.263 μM SANGER
HSC-2 Growth Inhibition Assay IC50=40.9113 μM SANGER
BxPC-3 Growth Inhibition Assay IC50=40.5686 μM SANGER
COLO-741 Growth Inhibition Assay IC50=40.1304 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=39.8274 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=39.5512 μM SANGER
MG-63 Growth Inhibition Assay IC50=39.3424 μM SANGER
EFO-21 Growth Inhibition Assay IC50=38.9349 μM SANGER
SW1417 Growth Inhibition Assay IC50=38.0552 μM SANGER
DU-4475 Growth Inhibition Assay IC50=36.9033 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=36.67 μM SANGER
Daoy Growth Inhibition Assay IC50=36.6538 μM SANGER
SW48 Growth Inhibition Assay IC50=36.2474 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=36.1198 μM SANGER
NB14 Growth Inhibition Assay IC50=34.4684 μM SANGER
COLO-800 Growth Inhibition Assay IC50=34.3647 μM SANGER
OE33 Growth Inhibition Assay IC50=34.2855 μM SANGER
CaR-1 Growth Inhibition Assay IC50=33.9822 μM SANGER
HT-144 Growth Inhibition Assay IC50=33.863 μM SANGER
LU-139 Growth Inhibition Assay IC50=33.6605 μM SANGER
SW626 Growth Inhibition Assay IC50=33.1776 μM SANGER
COR-L23 Growth Inhibition Assay IC50=32.9073 μM SANGER
769-P Growth Inhibition Assay IC50=32.3641 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=32.2897 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=31.8516 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=31.069 μM SANGER
DB Growth Inhibition Assay IC50=30.4942 μM SANGER
ZR-75-30 Growth Inhibition Assay IC50=30.2383 μM SANGER
HT-1197 Growth Inhibition Assay IC50=30.0598 μM SANGER
ES6 Growth Inhibition Assay IC50=29.8157 μM SANGER
PANC-03-27 Growth Inhibition Assay IC50=29.444 μM SANGER
ES7 Growth Inhibition Assay IC50=29.1465 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=28.5417 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=28.2964 μM SANGER
YAPC Growth Inhibition Assay IC50=28.2564 μM SANGER
CAL-12T Growth Inhibition Assay IC50=28.1112 μM SANGER
GI-1 Growth Inhibition Assay IC50=27.721 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=27.6012 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=27.4578 μM SANGER
SW948 Growth Inhibition Assay IC50=27.1344 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=27.0879 μM SANGER
SNU-449 Growth Inhibition Assay IC50=27.0803 μM SANGER
SW962 Growth Inhibition Assay IC50=26.5021 μM SANGER
CHP-134 Growth Inhibition Assay IC50=26.3867 μM SANGER
GMS-10 Growth Inhibition Assay IC50=26.2353 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=26.2103 μM SANGER
NB13 Growth Inhibition Assay IC50=26.0949 μM SANGER
EW-13 Growth Inhibition Assay IC50=26.0274 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=25.9945 μM SANGER
BT-549 Growth Inhibition Assay IC50=25.9011 μM SANGER
U-2-OS Growth Inhibition Assay IC50=25.6888 μM SANGER
HT-1376 Growth Inhibition Assay IC50=25.6465 μM SANGER
RH-18 Growth Inhibition Assay IC50=25.5918 μM SANGER
TE-1 Growth Inhibition Assay IC50=25.3563 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=25.1953 μM SANGER
MPP-89 Growth Inhibition Assay IC50=25.0458 μM SANGER
ALL-PO Growth Inhibition Assay IC50=24.619 μM SANGER
HCC2998 Growth Inhibition Assay IC50=24.4885 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=24.4874 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=24.3302 μM SANGER
DK-MG Growth Inhibition Assay IC50=24.294 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=24.2226 μM SANGER
HCC1806 Growth Inhibition Assay IC50=23.8709 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=23.8133 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=23.7759 μM SANGER
S-117 Growth Inhibition Assay IC50=23.7651 μM SANGER
DJM-1 Growth Inhibition Assay IC50=23.5234 μM SANGER
ES4 Growth Inhibition Assay IC50=23.4232 μM SANGER
M14 Growth Inhibition Assay IC50=23.4088 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=23.2533 μM SANGER
AM-38 Growth Inhibition Assay IC50=22.8689 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=22.764 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=22.3895 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=22.2432 μM SANGER
KU-19-19 Growth Inhibition Assay IC50=22.1697 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=22.034 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=21.7166 μM SANGER
KYSE-510 Growth Inhibition Assay IC50=21.6095 μM SANGER
CW-2 Growth Inhibition Assay IC50=21.6069 μM SANGER
LK-2 Growth Inhibition Assay IC50=21.5953 μM SANGER
22RV1 Growth Inhibition Assay IC50=21.5685 μM SANGER
HT-3 Growth Inhibition Assay IC50=21.5631 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=20.8134 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=20.7379 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=20.6883 μM SANGER
HT-1080 Growth Inhibition Assay IC50=20.5497 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=20.3374 μM SANGER
Mo-T Growth Inhibition Assay IC50=20.1665 μM SANGER
HL-60 Growth Inhibition Assay IC50=20.0941 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=20.0217 μM SANGER
TE-8 Growth Inhibition Assay IC50=19.3024 μM SANGER
8305C Growth Inhibition Assay IC50=19.2286 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=19.1546 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=19.0646 μM SANGER
NCI-N87 Growth Inhibition Assay IC50=18.9008 μM SANGER
A253 Growth Inhibition Assay IC50=18.7286 μM SANGER
KM-H2 Growth Inhibition Assay IC50=18.5232 μM SANGER
C32 Growth Inhibition Assay IC50=18.4727 μM SANGER
639-V Growth Inhibition Assay IC50=18.3354 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=18.2357 μM SANGER
EW-1 Growth Inhibition Assay IC50=18.1382 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=17.9673 μM SANGER
M059J Growth Inhibition Assay IC50=17.703 μM SANGER
KG-1 Growth Inhibition Assay IC50=17.6937 μM SANGER
KOSC-2 Growth Inhibition Assay IC50=17.6757 μM SANGER
UACC-257 Growth Inhibition Assay IC50=17.5512 μM SANGER
NH-12 Growth Inhibition Assay IC50=17.3303 μM SANGER
SW1783 Growth Inhibition Assay IC50=17.128 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=17.0707 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=17.0479 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=16.8419 μM SANGER
HCC1569 Growth Inhibition Assay IC50=16.8337 μM SANGER
Detroit562 Growth Inhibition Assay IC50=16.7318 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=16.6956 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=16.6373 μM SANGER
MDA-MB-453 Growth Inhibition Assay IC50=16.1642 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=15.7694 μM SANGER
SiHa Growth Inhibition Assay IC50=15.7594 μM SANGER
NCI-H727 Growth Inhibition Assay IC50=15.4221 μM SANGER
CAS-1 Growth Inhibition Assay IC50=15.4184 μM SANGER
OE19 Growth Inhibition Assay IC50=15.1541 μM SANGER
D-283MED Growth Inhibition Assay IC50=15.0111 μM SANGER
PC-14 Growth Inhibition Assay IC50=14.9654 μM SANGER
MS-1 Growth Inhibition Assay IC50=14.9611 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=14.7997 μM SANGER
CAL-120 Growth Inhibition Assay IC50=14.7027 μM SANGER
JEG-3 Growth Inhibition Assay IC50=14.6326 μM SANGER
NCI-H2291 Growth Inhibition Assay IC50=14.5878 μM SANGER
SW780 Growth Inhibition Assay IC50=14.5025 μM SANGER
BPH-1 Growth Inhibition Assay IC50=14.1664 μM SANGER
SCC-15 Growth Inhibition Assay IC50=13.9775 μM SANGER
CHP-212 Growth Inhibition Assay IC50=13.9739 μM SANGER
WM-115 Growth Inhibition Assay IC50=13.6483 μM SANGER
CTV-1 Growth Inhibition Assay IC50=13.345 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=13.2327 μM SANGER
HCC1187 Growth Inhibition Assay IC50=13.1912 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=12.9115 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=12.9041 μM SANGER
KYSE-140 Growth Inhibition Assay IC50=12.8595 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=12.5869 μM SANGER
GCIY Growth Inhibition Assay IC50=12.5209 μM SANGER
BCPAP Growth Inhibition Assay IC50=12.4749 μM SANGER
RH-1 Growth Inhibition Assay IC50=12.2184 μM SANGER
RPMI-7951 Growth Inhibition Assay IC50=12.1854 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=12.1177 μM SANGER
CAL-51 Growth Inhibition Assay IC50=12.0716 μM SANGER
EKVX Growth Inhibition Assay IC50=12.0313 μM SANGER
CFPAC-1 Growth Inhibition Assay IC50=11.9782 μM SANGER
D-247MG Growth Inhibition Assay IC50=11.9663 μM SANGER
GCT Growth Inhibition Assay IC50=11.8228 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=11.8093 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=11.7982 μM SANGER
MEG-01 Growth Inhibition Assay IC50=11.7509 μM SANGER
A427 Growth Inhibition Assay IC50=11.7093 μM SANGER
ONS-76 Growth Inhibition Assay IC50=11.636 μM SANGER
PC-3 Growth Inhibition Assay IC50=11.5764 μM SANGER
SW756 Growth Inhibition Assay IC50=11.5294 μM SANGER
TK10 Growth Inhibition Assay IC50=11.5271 μM SANGER
SW954 Growth Inhibition Assay IC50=11.4668 μM SANGER
DEL Growth Inhibition Assay IC50=11.424 μM SANGER
A388 Growth Inhibition Assay IC50=11.3897 μM SANGER
SF539 Growth Inhibition Assay IC50=10.9041 μM SANGER
no-11 Growth Inhibition Assay IC50=10.4353 μM SANGER
A549 Growth Inhibition Assay IC50=10.3973 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=10.2433 μM SANGER
LAN-6 Growth Inhibition Assay IC50=10.2164 μM SANGER
YKG-1 Growth Inhibition Assay IC50=10.2006 μM SANGER
A101D Growth Inhibition Assay IC50=9.99974 μM SANGER
MDA-MB-157 Growth Inhibition Assay IC50=9.92878 μM SANGER
5637 Growth Inhibition Assay IC50=9.84984 μM SANGER
A431 Growth Inhibition Assay IC50=9.80238 μM SANGER
U251 Growth Inhibition Assay IC50=9.65544 μM SANGER
ACN Growth Inhibition Assay IC50=9.53277 μM SANGER
SHP-77 Growth Inhibition Assay IC50=9.39935 μM SANGER
LS-123 Growth Inhibition Assay IC50=9.31761 μM SANGER
NBsusSR Growth Inhibition Assay IC50=9.27402 μM SANGER
DSH1 Growth Inhibition Assay IC50=9.2087 μM SANGER
HN Growth Inhibition Assay IC50=9.16628 μM SANGER
EFO-27 Growth Inhibition Assay IC50=9.16412 μM SANGER
8505C Growth Inhibition Assay IC50=9.04232 μM SANGER
NB10 Growth Inhibition Assay IC50=9.02224 μM SANGER
HEC-1 Growth Inhibition Assay IC50=8.89866 μM SANGER
ESS-1 Growth Inhibition Assay IC50=8.88704 μM SANGER
D-502MG Growth Inhibition Assay IC50=8.78629 μM SANGER
CAMA-1 Growth Inhibition Assay IC50=8.77146 μM SANGER
SCC-4 Growth Inhibition Assay IC50=8.68219 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=8.64696 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=8.64643 μM SANGER
SKG-IIIa Growth Inhibition Assay IC50=8.63069 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=8.53257 μM SANGER
SF126 Growth Inhibition Assay IC50=8.45936 μM SANGER
HCC1954 Growth Inhibition Assay IC50=8.45104 μM SANGER
T98G Growth Inhibition Assay IC50=8.18067 μM SANGER
JVM-3 Growth Inhibition Assay IC50=8.15268 μM SANGER
D-566MG Growth Inhibition Assay IC50=8.04429 μM SANGER
TE-5 Growth Inhibition Assay IC50=7.79334 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=7.67336 μM SANGER
CAL-33 Growth Inhibition Assay IC50=7.66233 μM SANGER
GB-1 Growth Inhibition Assay IC50=7.54804 μM SANGER
GP5d Growth Inhibition Assay IC50=7.48764 μM SANGER
MC-IXC Growth Inhibition Assay IC50=7.48576 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=7.2924 μM SANGER
LU-99A Growth Inhibition Assay IC50=7.14322 μM SANGER
SW1463 Growth Inhibition Assay IC50=7.11168 μM SANGER
RD Growth Inhibition Assay IC50=6.98284 μM SANGER
AU565 Growth Inhibition Assay IC50=6.96957 μM SANGER
TE-6 Growth Inhibition Assay IC50=6.93038 μM SANGER
TE-12 Growth Inhibition Assay IC50=6.83817 μM SANGER
A498 Growth Inhibition Assay IC50=6.81961 μM SANGER
CHL-1 Growth Inhibition Assay IC50=6.80079 μM SANGER
LN-405 Growth Inhibition Assay IC50=6.79672 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=6.63604 μM SANGER
A704 Growth Inhibition Assay IC50=6.6306 μM SANGER
SNB75 Growth Inhibition Assay IC50=6.60143 μM SANGER
D-263MG Growth Inhibition Assay IC50=6.45169 μM SANGER
NB12 Growth Inhibition Assay IC50=6.39071 μM SANGER
BFTC-909 Growth Inhibition Assay IC50=6.30345 μM SANGER
BT-474 Growth Inhibition Assay IC50=6.233 μM SANGER
EW-22 Growth Inhibition Assay IC50=6.19649 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=6.08773 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=5.99816 μM SANGER
Saos-2 Growth Inhibition Assay IC50=5.8653 μM SANGER
Becker Growth Inhibition Assay IC50=5.86472 μM SANGER
SF295 Growth Inhibition Assay IC50=5.80633 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=5.72732 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=5.66199 μM SANGER
SW872 Growth Inhibition Assay IC50=5.59428 μM SANGER
CAL-27 Growth Inhibition Assay IC50=5.46339 μM SANGER
MEL-HO Growth Inhibition Assay IC50=5.37336 μM SANGER
BT-20 Growth Inhibition Assay IC50=5.21353 μM SANGER
ETK-1 Growth Inhibition Assay IC50=5.21165 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=5.20009 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=4.96142 μM SANGER
786-0 Growth Inhibition Assay IC50=4.94673 μM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=4.942 μM SANGER
TI-73 Growth Inhibition Assay IC50=4.80609 μM SANGER
CAL-39 Growth Inhibition Assay IC50=4.72146 μM SANGER
KLE Growth Inhibition Assay IC50=4.70198 μM SANGER
NB5 Growth Inhibition Assay IC50=4.53697 μM SANGER
ATN-1 Growth Inhibition Assay IC50=4.44304 μM SANGER
EW-11 Growth Inhibition Assay IC50=4.41838 μM SANGER
HCE-T Growth Inhibition Assay IC50=4.41579 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=4.38146 μM SANGER
EGI-1 Growth Inhibition Assay IC50=4.37778 μM SANGER
NCI-H460 Growth Inhibition Assay IC50=4.26443 μM SANGER
Calu-3 Growth Inhibition Assay IC50=4.24416 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=4.14191 μM SANGER
TYK-nu Growth Inhibition Assay IC50=4.09534 μM SANGER
SCC-25 Growth Inhibition Assay IC50=4.06566 μM SANGER
MLMA Growth Inhibition Assay IC50=4.02966 μM SANGER
TGW Growth Inhibition Assay IC50=4.02305 μM SANGER
ECC10 Growth Inhibition Assay IC50=3.93622 μM SANGER
LU-134-A Growth Inhibition Assay IC50=3.88428 μM SANGER
RVH-421 Growth Inhibition Assay IC50=3.81788 μM SANGER
P30-OHK Growth Inhibition Assay IC50=3.80976 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=3.72038 μM SANGER
G-402 Growth Inhibition Assay IC50=3.70711 μM SANGER
SJRH30 Growth Inhibition Assay IC50=3.69122 μM SANGER
KNS-62 Growth Inhibition Assay IC50=3.63338 μM SANGER
AN3-CA Growth Inhibition Assay IC50=3.62456 μM SANGER
DMS-114 Growth Inhibition Assay IC50=3.62278 μM SANGER
RT-112 Growth Inhibition Assay IC50=3.52388 μM SANGER
SW1710 Growth Inhibition Assay IC50=3.46678 μM SANGER
H4 Growth Inhibition Assay IC50=3.45626 μM SANGER
NCI-H1623 Growth Inhibition Assay IC50=3.41224 μM SANGER
OVCAR-3 Growth Inhibition Assay IC50=3.40786 μM SANGER
HCC2157 Growth Inhibition Assay IC50=3.38179 μM SANGER
DOK Growth Inhibition Assay IC50=3.22859 μM SANGER
EW-16 Growth Inhibition Assay IC50=3.21879 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=3.20694 μM SANGER
EW-3 Growth Inhibition Assay IC50=3.19529 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=3.1119 μM SANGER
HuH-7 Growth Inhibition Assay IC50=3.09464 μM SANGER
EoL-1- Growth Inhibition Assay IC50=3.07058 μM SANGER
GR-ST Growth Inhibition Assay IC50=3.04611 μM SANGER
NCI-H1048 Growth Inhibition Assay IC50=2.96865 μM SANGER
SNU-423 Growth Inhibition Assay IC50=2.89242 μM SANGER
MCF7 Growth Inhibition Assay IC50=2.86117 μM SANGER
A204 Growth Inhibition Assay IC50=2.83872 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=2.75266 μM SANGER
HCC1395 Growth Inhibition Assay IC50=2.75187 μM SANGER
AGS Growth Inhibition Assay IC50=2.72137 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=2.62953 μM SANGER
RXF393 Growth Inhibition Assay IC50=2.60487 μM SANGER
ES3 Growth Inhibition Assay IC50=2.49759 μM SANGER
ES8 Growth Inhibition Assay IC50=2.49287 μM SANGER
T-24 Growth Inhibition Assay IC50=2.47881 μM SANGER
YH-13 Growth Inhibition Assay IC50=2.46153 μM SANGER
EW-18 Growth Inhibition Assay IC50=2.41939 μM SANGER
D-423MG Growth Inhibition Assay IC50=2.41044 μM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=2.39083 μM SANGER
NB69 Growth Inhibition Assay IC50=2.38983 μM SANGER
KS-1 Growth Inhibition Assay IC50=2.38191 μM SANGER
LS-513 Growth Inhibition Assay IC50=2.33484 μM SANGER
ABC-1 Growth Inhibition Assay IC50=2.33253 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=2.31552 μM SANGER
OAW-28 Growth Inhibition Assay IC50=2.29951 μM SANGER
MN-60 Growth Inhibition Assay IC50=2.29923 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=2.24317 μM SANGER
GAMG Growth Inhibition Assay IC50=2.23845 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=2.18091 μM SANGER
RMG-I Growth Inhibition Assay IC50=2.16398 μM SANGER
OC-314 Growth Inhibition Assay IC50=2.15086 μM SANGER
Hs-578-T Growth Inhibition Assay IC50=2.11433 μM SANGER
SW1088 Growth Inhibition Assay IC50=1.94606 μM SANGER
SNU-387 Growth Inhibition Assay IC50=1.88406 μM SANGER
RKO Growth Inhibition Assay IC50=1.87101 μM SANGER
BV-173 Growth Inhibition Assay IC50=1.81074 μM SANGER
COR-L105 Growth Inhibition Assay IC50=1.79737 μM SANGER
OMC-1 Growth Inhibition Assay IC50=1.74677 μM SANGER
CAL-54 Growth Inhibition Assay IC50=1.71242 μM SANGER
HCC2218 Growth Inhibition Assay IC50=1.68225 μM SANGER
ME-180 Growth Inhibition Assay IC50=1.56891 μM SANGER
DMS-273 Growth Inhibition Assay IC50=1.51959 μM SANGER
HOS Growth Inhibition Assay IC50=1.49558 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=1.49116 μM SANGER
697 Growth Inhibition Assay IC50=1.37616 μM SANGER
PA-1 Growth Inhibition Assay IC50=1.35265 μM SANGER
MFM-223 Growth Inhibition Assay IC50=1.34461 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=1.33701 μM SANGER
LoVo Growth Inhibition Assay IC50=1.32534 μM SANGER
G-401 Growth Inhibition Assay IC50=1.29795 μM SANGER
CTB-1 Growth Inhibition Assay IC50=1.2899 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=1.28203 μM SANGER
ES1 Growth Inhibition Assay IC50=1.24065 μM SANGER
COLO-684 Growth Inhibition Assay IC50=1.23725 μM SANGER
EPLC-272H Growth Inhibition Assay IC50=1.17256 μM SANGER
LXF-289 Growth Inhibition Assay IC50=1.17156 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=1.14485 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=0.99734 μM SANGER
NCI-H520 Growth Inhibition Assay IC50=0.98592 μM SANGER
EM-2 Growth Inhibition Assay IC50=0.97939 μM SANGER
MFE-280 Growth Inhibition Assay IC50=0.96465 μM SANGER
HuO9 Growth Inhibition Assay IC50=0.92751 μM SANGER
OAW-42 Growth Inhibition Assay IC50=0.8872 μM SANGER
HOP-92 Growth Inhibition Assay IC50=0.87223 μM SANGER
NKM-1 Growth Inhibition Assay IC50=0.86253 μM SANGER
L-363 Growth Inhibition Assay IC50=0.83442 μM SANGER
NB7 Growth Inhibition Assay IC50=0.82411 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=0.80582 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=0.74403 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=0.73025 μM SANGER
OCUB-M Growth Inhibition Assay IC50=0.70966 μM SANGER
DU-145 Growth Inhibition Assay IC50=0.64745 μM SANGER
NOS-1 Growth Inhibition Assay IC50=0.63723 μM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=0.63626 μM SANGER
HT Growth Inhibition Assay IC50=0.63239 μM SANGER
HAL-01 Growth Inhibition Assay IC50=0.6213 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=0.61048 μM SANGER
HCC70 Growth Inhibition Assay IC50=0.59827 μM SANGER
KE-37 Growth Inhibition Assay IC50=0.5826 μM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=0.57761 μM SANGER
HGC-27 Growth Inhibition Assay IC50=0.56783 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=0.55249 μM SANGER
BHT-101 Growth Inhibition Assay IC50=0.52961 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=0.49939 μM SANGER
HCC1419 Growth Inhibition Assay IC50=0.48892 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=0.48189 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=0.46868 μM SANGER
SBC-1 Growth Inhibition Assay IC50=0.44035 μM SANGER
EFM-19 Growth Inhibition Assay IC50=0.4401 μM SANGER
H9 Growth Inhibition Assay IC50=0.38883 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=0.37679 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=0.37321 μM SANGER
RS4-11 Growth Inhibition Assay IC50=0.3461 μM SANGER
ES5 Growth Inhibition Assay IC50=0.34455 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=0.3032 μM SANGER
HH Growth Inhibition Assay IC50=0.30283 μM SANGER
T47D Growth Inhibition Assay IC50=0.2825 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=0.22122 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=0.13738 μM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=0.1162 μM SANGER
NEC8 Growth Inhibition Assay IC50=0.09651 μM SANGER
HONE-1 Function Assay 10 μM 48 h DMSO Induces cell cycle arrest at G1 25336925
CNE-2 Function Assay 10 μM 48 h DMSO Induces cell cycle arrest at G1 25336925
HONE-1 Growth Inhibition Assay 10 μM 96 h DMSO IC50=3.37 μM 25336925
SUNE-1 Growth Inhibition Assay 10 μM 96 h DMSO IC50=0.52 μM 25336925
CNE-2 Growth Inhibition Assay 10 μM 96 h DMSO IC50=4.53 μM 25336925
CNE-1 Growth Inhibition Assay 10 μM 96 h DMSO IC50=2.96 μM 25336925
GEO Growth Inhibition Assay 500 nM 72 h DMSO Inhibits cell growth 24581231
HepG2 cell Apoptosis Assay 20 μM 24 h DMSO Induces cell apoptosis 23797319
HepG2 cell Growth Inhibition Assay 30 μM 24 h DMSO Inhibits cell growth 23797319
HepG2 cell Kinase Assay 20 μM 24 h DMSO Downregulates the phosphorylation of AKT 23797319
CEM-S Function Assay 4 μM 4 h DMSO Increases the amount of cleaved LC5A/B, a well-established autophagy marker 22614243
CEM-R Function Assay 4 μM 4 h DMSO Increases the amount of cleaved LC4A/B, a well-established autophagy marker 22614243
MOLT-4 Function Assay 4 μM 4 h DMSO Increases the amount of cleaved LC3A/B, a well-established autophagy marker 22614243
MOLT-4 Function Assay 10 μM 24 h DMSO Blocks cells in the G0/G1 phase of the cell cycle 22614243
CEM-S Cytotoxic Assay 10 μM 48 h DMSO IC50=5.1 μM 22614243
CEM-R Cytotoxic Assay 10 μM 48 h DMSO IC50=3.3 μM 22614243
MOLT-4 Cytotoxic Assay 10 μM 48 h DMSO IC50=1.7 μM 22614243
HC11 Function Assay 10 μM 24 h DMSO Inhibits β-casein and ADRP synthesis 22426621
T98G Apoptosis Assay 0.5 μM 60 h DMSO Augments apoptogenic effects of gefitinib 22057914
TAD2 Growth Inhibition Assay 1000 μM 5 d DMSO IC50>1000 μM 21289267
LN229 Apoptosis Assay 0.5 μM 60 h DMSO Augments apoptogenic effects of gefitinib 22057914
WRO Growth Inhibition Assay 1000 μM 5 d DMSO IC50>1000 μM 21289267
SW1736 Growth Inhibition Assay 100 μM 5 d DMSO IC50=47.56 μM 21289267
KAT18 Growth Inhibition Assay 3 μM 5 d DMSO IC50=4.62 μM 21289267
Hth74 Growth Inhibition Assay 3 μM 5 d DMSO IC50=2.19 μM 21289267
TPC1 cells harbored RET/PTC1 rearrangement Growth Inhibition Assay 3 μM 5 d DMSO IC50=0.59 μM 21289267
Hth7 cells harbored NRAS (Q61R+/−) Growth Inhibition Assay 3 μM 5 d DMSO IC50=4.5 μM 21289267
C643 cells harbored HRAS (G13R+/−) Growth Inhibition Assay 3 μM 5 d DMSO IC50=0.27 μM 21289267
FTC133 cells harbored PTEN (allele deletion and R130+) Growth Inhibition Assay 3 μM 5 d DMSO IC50=0.18 μM 21289267
K1 cells harbored PIK3CA (E542K+/+) Growth Inhibition Assay 3 μM 5 d DMSO IC50=0.52 μM 21289267
OCUT1 cells harbored PIK3CA (H1047R+/+) Growth Inhibition Assay 3 μM 5 d DMSO IC50=0.14 μM 21289267
Sk-Hep1 Cytotoxic Assay 10 μM 24 h DMSO Sensitizes resistant cells to the cytotoxic effect of sorafenib 21205925
HepG2 Cytotoxic Assay 10 μM 24 h DMSO Sensitizes resistant cells to the cytotoxic effect of sorafenib 21205925
A431 Kinase Assay 5 μM 5 h DMSO Suppresses the signaling of Akt and Erk 20571069
NCI-H292 Cytotoxic Assay 3 μM 72 h DMSO Inhibition of cell proliferation 20571069
HeLa Function assay 1 h IC50 = 0.0228 μM 29100733
NCI-H460 Growth inhibition assay 72 h IC50 = 5.4 μM 24900862
HCT116 Growth inhibition assay 72 h IC50 = 7.5 μM 24900862
A673 Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
MG 63 (6-TG R) Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
Rh30 Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
SJ-GBM2 Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 Function assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.
Features The first allosteric small molecule inhibitor of Akt to enter clinical development.
Targets
Akt1 [1]
(Cell-free assay)		 Akt2 [1]
(Cell-free assay)		 Akt3 [1]
(Cell-free assay)
8 nM 12 nM 65 nM
In vitro
In vitro MK-2206 is an allosteric inhibitor and is activated by the pleckstrin homology domain. MK-2206 inhibits auto-phosphorylation of both Akt T308 and S473. MK-2206 also prevents Akt-mediated phosphorylation of downstream signaling molecules, including TSC2, PRAS40 and ribosomal S6 proteins. [1] MK-2206 inhibits Ras wild-type (WT) cell lines (A431, HCC827, and NCI-H292) more potently when compared to Ras-mutant cell lines (NCI-H358, NCI-H23, NCI-H1299, and Calu-6). MK-2206 also shows synergistic responses in combination with cytotoxic agents such as erlotinib or lapatinib in lung NCI-H460 or ovarian A2780 tumor cells. [2] MK-2206 or siRNA-mediated Akt inhibition strongly activates autophagy in human glioma cells. However, eukaryotic elongation factor-2 (eEF-2) silencing suppresses MK-2206-induced-autophagy, with a promotion of apoptotic cell death. [3]
Kinase Assay Akt kinases assay
Akt kinases are assayed by a GSK-derived biotinylated peptide substrate. The extent of peptide phosphorylation is determined by Homogeneous Time Resolved Fluorescence (HTRF) using a lanthanide chelate (Lance)-coupled monoclonal antibody specific for the phosphopeptide in combination with a streptavidin-linked allophycocyanin (SA-APC) fluorophore which will bind to the biotin moiety on the peptide. When the Lance and APC are in proximity, a non-radiative energy transfer takes place from the Lance to the APC, followed by emission of light from APC at 655 nm. Working Solution: 100X protease inhibitor cocktail (PIC): 1mg/mL benzamidine, 0.5 mg/mL pepstatin, 0.5 mg/mL leupeptin, 0.5 mg/mL aprotinin; 10X assay buffer: 500 mM HEPES, pH7.5, 1% PEG, 16.6 mM EDTA, 1 mM EGTA, 1% BSA, 20 mM 9-glycerol phosphate; Quench buffer 50 mM HEPES pH 7.3, 16.6 mM EDTA, 0.1% BSA, 0.1% Triton X-100, 0.17 nM labeled monoclonal antibody, 0.0067 mg/mL SA-APC; ATP/MgCl2 working solution: 1X Assay buffer, 1 mM DTT, 1X PIC, 5% glycerol, active Akt; Peptide working solution: 1X Assay buffer, 1 mM DTT, 1X PIC, 5% glycerol, 2 TM GSK biotinylated peptide. The reaction is assembled by adding 16 µL of ATP/MgCl2 working solution to the appropriate wells. MK-2206 or vehicle (1.0 µL) is added followed by 10 µL of peptide working solution. The reaction is started by adding 13 μL of the enzyme working solution and mixing. The reaction is allowed to proceed for 50 min and then stopped by the addition of 60 µL HTRF quench buffer. The stopped reactions are incubated at room temperature for at least 30 min and then read in the instrument.
Cell Research Cell lines A431, HCC827, NCI-H292, NCI-H358, NCI-H23, NCI-H1299, Calu-6 and NCI-H460 cells
Concentrations 0, 0.3, 1 and 3 μM
Incubation Time 72 or 96 hours
Method

MK-2206 is dissolved in DMSO as a stock solution and diluted by culture media before use. Cells are seeded at a density of 2-3 × 103 in 96-well plates and incubated for 24 hours. Then MK-2206 (0, 0.3, 1 and 3 μM) is added to the cells. Cell proliferation is determined after 72 or 96 hours.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AKT(T308) / p-AKT(S473) / pGSK3β(S9) / pFOXO1 / pPRAS(T246) / pBAD / pS6K(T389) / p4E-BP1 22932669
Growth inhibition assay Cell viability 24665203
Immunofluorescence LC3 CFTR/LC3 HMGA2 24490764
ELISA VEGFA 29449553
In Vivo
In vivo MK-2206 shows 60% TGI and inhibits more than 70 % of phospho-Akt1/2 (T308 and S473) in A2780 ovarian cancer xenografts at a dose of 240 mg/kg. [1] MK-2206 exhibits significant antitumor activity in NCI-H292 xenograft in combination with erlotinib or lapatinib. [2]
Animal Research Animal Models SK-OV-3, NCI-H292, HCC70, PC-3, and NCI-H460 models in male CD1-nude mice
Dosages 120 mg/kg
Administration Orally administered
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01480154 Active not recruiting Advanced Malignant Solid Neoplasm|Stage III Cutaneous Melanoma AJCC v7|Stage III Prostate Cancer AJCC v7|Stage III Renal Cell Cancer AJCC v7|Stage IIIA Cutaneous Melanoma AJCC v7|Stage IIIB Cutaneous Melanoma AJCC v7|Stage IIIC Cutaneous Melanoma AJCC v7|Stage IV Cutaneous Melanoma AJCC v6 and v7|Stage IV Prostate Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7 National Cancer Institute (NCI) November 23 2011 Phase 1
NCT01466868 Terminated Diffuse Large B Cell Lymphoma Centre Leon Berard|National Cancer Institute France November 2011 Phase 2

Chemical lnformation & Solubility

Molecular Weight 480.39 Formula

C25H21N5O.2HCl
CAS No. 1032350-13-2 SDF Download MK-2206 2HCl SDF
Smiles C1CC(C1)(C2=CC=C(C=C2)C3=C(C=C4C(=N3)C=CN5C4=NNC5=O)C6=CC=CC=C6)N.Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 96 mg/mL ( (199.83 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 96 mg/mL

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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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. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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.

Handling Instructions

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Frequently Asked Questions

Question 1:
What is your recommendation for preparing the solution and how would you deliver it to the mice (i.p. or gavage)?

Answer:
You can resuspend MK-2206 in 15% Captisol at up to 17mg/ml. It's a suspension and is for oral gavage use only.

Question 2:
I would want to know if MK-2206 could cross the blood brain barrier?

Answer:
MK-2206 can cross BBB based on the following reference: https://clinicaltrials.gov/ct2/show/NCT01249105.

Akt Signaling Pathway Map

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