Home Protein Tyrosine Kinase EGFR inhibitor - Autophagy activator - Apoptosis related activator Gefitinib For research use only.

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

Gefitinib Chemical Structure

CAS No. 184475-35-2

Purity & Quality Control

Gefitinib Related Products

Signaling Pathway

EGFR Signaling Pathways

EGFR Signaling Pathway

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
Tyr1173 (NR6W cells) [1] Tyr1173 (NR6wtEGFR cells) [1] Tyr992 (NR6wtEGFR cells) [1] Tyr992 (NR6W cells) [1]
26 nM 37 nM 37 nM 57 nM
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]
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.
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
 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 Information & 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
Batch:

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

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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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.

Handling Instructions

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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.

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