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Gefitinib

Name: Gefitinib
Brand: Selleck Chemicals
SKU: S1025
Rating: 5 (719 reviews)

Synonyms: ZD1839

Catalog No.S1025 Purity:99.98%

Gefitinib is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.

Gefitinib Chemical Structure

CAS No. 184475-35-2

Purity & Quality Control

Batch: Purity: 99.98%

99.98

Gefitinib Related Products

Related Targets	EGFR/ErbB1 HER2/ErbB2 ErbB3 ErbB4 mutant EGFR	Click to Expand
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Related Compound Libraries	Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library PI3K/Akt Inhibitor Library Cell Cycle compound library Angiogenesis Related compound Library	Click to Expand

Signaling Pathway

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

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	PPAR-γ uc-caspase-9 / c-caspase-9 / uc-caspase-3 / c-caspase-3 / uc-PARP / PARP Cyclin D1/ p16 / p27 / pRb phospho-EGFR / phospho-ERK / phospho-SRC / phospho-AKT		23409107
	Immunofluorescence	p-EGFR / β-catenin PPAR-γ EGFR / LC3		23461856
	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

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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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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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