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Afatinib (BIBW 2992)

(CAS No:439081-18-2)
Afatinib (BIBW2992) irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM in cell-free assays, respectively.
CAS No:439081-18-2
Molecular Weight(MW):485.94
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 439081-18-2
Molecular formula(MF) C24H25ClFN5O3
Molecular Weight(MW): 485.94
Alias BIBW 2992
Solubility
In vitro DMSO 97 mg/mL (199.61 mM)
Ethanol 15 mg/mL (30.86 mM)
Water <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 10mg/mL
Biological Activity
Description Afatinib (BIBW2992) irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM in cell-free assays, respectively.
Targets
EGFR (L858R) [1]
(Cell-free assay)
EGFR (wt) [1]
(Cell-free assay)
EGFR (L858R/T790M) [1]
(Cell-free assay)
HER2 [1]
(Cell-free assay)
0.4 nM 0.5 nM 10 nM 14 nM
In vitro

BIBW2992 shows potent activity against both wild-type and mutant forms of EGFR and HER2. It is similar to Gefitinib in potency against L858R EGFR, but about 100-fold more active against the Gefitinib resistant L858R-T790M EGFR double mutant. BIBW2992 exhibits potent effects on both EGFR and HER2 phosphorylation in vivo. It compares favorably to reference compounds (such as Lapatinib et al.) in all cell types tested, such as human epidermoid carcinoma cell line A431 expressing wt EGFR, murine NIH-3T3 cells transfected with wt HER2, as well as breast cancer cell line BT-474 and gastric cancer cell line NCI-N87, which express endogenous HER2. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HDLM-2 Growth Inhibition Assay IC50=0.00572 μM SANGER
KASUMI-1 Growth Inhibition Assay IC50=0.00911 μM SANGER
HCC2218 Growth Inhibition Assay IC50=0.00987 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=0.01671 μM SANGER
HSC-4 Growth Inhibition Assay IC50=0.01748 μM SANGER
CHL-1 Growth Inhibition Assay IC50=0.01839 μM SANGER
KY821 Growth Inhibition Assay IC50=0.0206 μM SANGER
NCI-N87 Growth Inhibition Assay IC50=0.02773 μM SANGER
DOK Growth Inhibition Assay IC50=0.03194 μM SANGER
DSH1 Growth Inhibition Assay IC50=0.03314 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=0.03416 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=0.03728 μM SANGER
BT-474 Growth Inhibition Assay IC50=0.04986 μM SANGER
EFO-27 Growth Inhibition Assay IC50=0.05182 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=0.05325 μM SANGER
PC-14 Growth Inhibition Assay IC50=0.05668 μM SANGER
EC-GI-10 Growth Inhibition Assay IC50=0.05912 μM SANGER
KYSE-450 Growth Inhibition Assay IC50=0.05978 μM SANGER
BPH-1 Growth Inhibition Assay IC50=0.05988 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=0.0609 μM SANGER
H9 Growth Inhibition Assay IC50=0.07132 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=0.07823 μM SANGER
NCI-H1623 Growth Inhibition Assay IC50=0.08025 μM SANGER
KYSE-140 Growth Inhibition Assay IC50=0.0833 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=0.08353 μM SANGER
AU565 Growth Inhibition Assay IC50=0.08504 μM SANGER
ZR-75-30 Growth Inhibition Assay IC50=0.09545 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=0.1028 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=0.10884 μM SANGER
CAL-39 Growth Inhibition Assay IC50=0.11792 μM SANGER
UACC-893 Growth Inhibition Assay IC50=0.11885 μM SANGER
LU-65 Growth Inhibition Assay IC50=0.12633 μM SANGER
HN Growth Inhibition Assay IC50=0.13077 μM SANGER
TI-73 Growth Inhibition Assay IC50=0.14715 μM SANGER
KU812 Growth Inhibition Assay IC50=0.15456 μM SANGER
SW13 Growth Inhibition Assay IC50=0.16216 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=0.16576 μM SANGER
HSC-2 Growth Inhibition Assay IC50=0.16837 μM SANGER
BV-173 Growth Inhibition Assay IC50=0.17596 μM SANGER
CAL-27 Growth Inhibition Assay IC50=0.17636 μM SANGER
SBC-1 Growth Inhibition Assay IC50=0.18959 μM SANGER
CAL-33 Growth Inhibition Assay IC50=0.20184 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=0.2046 μM SANGER
COR-L105 Growth Inhibition Assay IC50=0.21084 μM SANGER
HSC-3 Growth Inhibition Assay IC50=0.21198 μM SANGER
NCI-H69 Growth Inhibition Assay IC50=0.21451 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=0.23975 μM SANGER
ML-2 Growth Inhibition Assay IC50=0.24802 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=0.25952 μM SANGER
TK10 Growth Inhibition Assay IC50=0.26738 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=0.26892 μM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=0.27853 μM SANGER
BHY Growth Inhibition Assay IC50=0.28655 μM SANGER
LU-139 Growth Inhibition Assay IC50=0.3051 μM SANGER
23132-87 Growth Inhibition Assay IC50=0.31923 μM SANGER
ACHN Growth Inhibition Assay IC50=0.31994 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=0.32219 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=0.34593 μM SANGER
HLE Growth Inhibition Assay IC50=0.35046 μM SANGER
HCC1419 Growth Inhibition Assay IC50=0.36408 μM SANGER
A388 Growth Inhibition Assay IC50=0.36857 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=0.38373 μM SANGER
KYSE-180 Growth Inhibition Assay IC50=0.39089 μM SANGER
TE-6 Growth Inhibition Assay IC50=0.40246 μM SANGER
A498 Growth Inhibition Assay IC50=0.40674 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=0.44182 μM SANGER
DU-145 Growth Inhibition Assay IC50=0.44833 μM SANGER
CW-2 Growth Inhibition Assay IC50=0.46914 μM SANGER
A431 Growth Inhibition Assay IC50=0.48233 μM SANGER
SAS Growth Inhibition Assay IC50=0.48398 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=0.51926 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=0.5321 μM SANGER
FADU Growth Inhibition Assay IC50=0.54404 μM SANGER
ACN Growth Inhibition Assay IC50=0.55094 μM SANGER
HCC70 Growth Inhibition Assay IC50=0.57661 μM SANGER
NCI-H1838 Growth Inhibition Assay IC50=0.60299 μM SANGER
CAL-54 Growth Inhibition Assay IC50=0.61621 μM SANGER
NCI-H1975 Growth Inhibition Assay IC50=0.61728 μM SANGER
COR-L88 Growth Inhibition Assay IC50=0.64113 μM SANGER
CTV-1 Growth Inhibition Assay IC50=0.64392 μM SANGER
EW-18 Growth Inhibition Assay IC50=0.68698 μM SANGER
HCC1806 Growth Inhibition Assay IC50=0.69666 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=0.6976 μM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=0.72662 μM SANGER
NCI-H1573 Growth Inhibition Assay IC50=0.7363 μM SANGER
KU-19-19 Growth Inhibition Assay IC50=0.77464 μM SANGER
COLO-678 Growth Inhibition Assay IC50=0.80834 μM SANGER
C-33-A Growth Inhibition Assay IC50=0.81297 μM SANGER
Calu-3 Growth Inhibition Assay IC50=0.81434 μM SANGER
AGS Growth Inhibition Assay IC50=0.83648 μM SANGER
SCC-25 Growth Inhibition Assay IC50=0.84171 μM SANGER
JVM-2 Growth Inhibition Assay IC50=0.88299 μM SANGER
HCE-T Growth Inhibition Assay IC50=0.88428 μM SANGER
ES4 Growth Inhibition Assay IC50=0.97836 μM SANGER
EKVX Growth Inhibition Assay IC50=1.01064 μM SANGER
D-542MG Growth Inhibition Assay IC50=1.01064 μM SANGER
SW1116 Growth Inhibition Assay IC50=1.01287 μM SANGER
5637 Growth Inhibition Assay IC50=1.0151 μM SANGER
HT-1376 Growth Inhibition Assay IC50=1.01513 μM SANGER
NB69 Growth Inhibition Assay IC50=1.02945 μM SANGER
YKG-1 Growth Inhibition Assay IC50=1.05419 μM SANGER
EW-3 Growth Inhibition Assay IC50=1.07883 μM SANGER
GCIY Growth Inhibition Assay IC50=1.08104 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=1.11487 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=1.16416 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=1.17513 μM SANGER
SW954 Growth Inhibition Assay IC50=1.20214 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=1.239 μM SANGER
SW48 Growth Inhibition Assay IC50=1.25432 μM SANGER
HT-3 Growth Inhibition Assay IC50=1.28753 μM SANGER
ETK-1 Growth Inhibition Assay IC50=1.37456 μM SANGER
SCC-15 Growth Inhibition Assay IC50=1.39451 μM SANGER
DU-4475 Growth Inhibition Assay IC50=1.40121 μM SANGER
NB5 Growth Inhibition Assay IC50=1.41317 μM SANGER
CFPAC-1 Growth Inhibition Assay IC50=1.42493 μM SANGER
NCI-H630 Growth Inhibition Assay IC50=1.45582 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=1.54006 μM SANGER
ECC10 Growth Inhibition Assay IC50=1.55369 μM SANGER
K5 Growth Inhibition Assay IC50=1.58357 μM SANGER
ME-180 Growth Inhibition Assay IC50=1.61096 μM SANGER
KYSE-410 Growth Inhibition Assay IC50=1.65672 μM SANGER
G-401 Growth Inhibition Assay IC50=1.67413 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=1.6823 μM SANGER
Detroit562 Growth Inhibition Assay IC50=1.70152 μM SANGER
OE19 Growth Inhibition Assay IC50=1.71512 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=1.78211 μM SANGER
TE-12 Growth Inhibition Assay IC50=1.80414 μM SANGER
NCI-H1666 Growth Inhibition Assay IC50=1.80948 μM SANGER
TE-1 Growth Inhibition Assay IC50=1.81475 μM SANGER
CAL-12T Growth Inhibition Assay IC50=1.88945 μM SANGER
TE-8 Growth Inhibition Assay IC50=1.91377 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=2.02732 μM SANGER
GMS-10 Growth Inhibition Assay IC50=2.03517 μM SANGER
A2780 Growth Inhibition Assay IC50=2.06294 μM SANGER
OMC-1 Growth Inhibition Assay IC50=2.08169 μM SANGER
LoVo Growth Inhibition Assay IC50=2.10797 μM SANGER
PANC-03-27 Growth Inhibition Assay IC50=2.16631 μM SANGER
MDA-MB-157 Growth Inhibition Assay IC50=2.21828 μM SANGER
CaR-1 Growth Inhibition Assay IC50=2.28281 μM SANGER
769-P Growth Inhibition Assay IC50=2.29037 μM SANGER
NB7 Growth Inhibition Assay IC50=2.29676 μM SANGER
MKN7 Growth Inhibition Assay IC50=2.35335 μM SANGER
NCI-H1048 Growth Inhibition Assay IC50=2.49158 μM SANGER
RCM-1 Growth Inhibition Assay IC50=2.52938 μM SANGER
HT55 Growth Inhibition Assay IC50=2.5738 μM SANGER
HCC1569 Growth Inhibition Assay IC50=2.58297 μM SANGER
LXF-289 Growth Inhibition Assay IC50=2.63565 μM SANGER
OVCAR-3 Growth Inhibition Assay IC50=2.67167 μM SANGER
TE-10 Growth Inhibition Assay IC50=2.68078 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=2.68616 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=2.74888 μM SANGER
SN12C Growth Inhibition Assay IC50=2.91964 μM SANGER
786-0 Growth Inhibition Assay IC50=3.06408 μM SANGER
HT-29 Growth Inhibition Assay IC50=3.07309 μM SANGER
RPMI-7951 Growth Inhibition Assay IC50=3.0759 μM SANGER
NBsusSR Growth Inhibition Assay IC50=3.18254 μM SANGER
NKM-1 Growth Inhibition Assay IC50=3.18744 μM SANGER
Capan-2 Growth Inhibition Assay IC50=3.46875 μM SANGER
MKN1 Growth Inhibition Assay IC50=3.47108 μM SANGER
OAW-42 Growth Inhibition Assay IC50=3.50026 μM SANGER
SKG-IIIa Growth Inhibition Assay IC50=3.52237 μM SANGER
no-11 Growth Inhibition Assay IC50=3.53564 μM SANGER
NY Growth Inhibition Assay IC50=3.53655 μM SANGER
HEC-1 Growth Inhibition Assay IC50=3.5895 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=3.59841 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=3.61216 μM SANGER
T47D Growth Inhibition Assay IC50=3.62217 μM SANGER
SNU-449 Growth Inhibition Assay IC50=3.65826 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=3.69735 μM SANGER
BT-20 Growth Inhibition Assay IC50=3.69795 μM SANGER
LS-123 Growth Inhibition Assay IC50=3.74284 μM SANGER
8305C Growth Inhibition Assay IC50=3.75911 μM SANGER
OCUB-M Growth Inhibition Assay IC50=3.76187 μM SANGER
KOSC-2 Growth Inhibition Assay IC50=3.83451 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=3.84181 μM SANGER
TE-9 Growth Inhibition Assay IC50=3.84382 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=3.87994 μM SANGER
GAMG Growth Inhibition Assay IC50=3.91314 μM SANGER
KNS-62 Growth Inhibition Assay IC50=3.94731 μM SANGER
MC116 Growth Inhibition Assay IC50=3.95489 μM SANGER
647-V Growth Inhibition Assay IC50=3.98452 μM SANGER
U-87-MG Growth Inhibition Assay IC50=4.10481 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=4.11631 μM SANGER
SW1417 Growth Inhibition Assay IC50=4.12147 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=4.1702 μM SANGER
LS-513 Growth Inhibition Assay IC50=4.31217 μM SANGER
KLE Growth Inhibition Assay IC50=4.40819 μM SANGER
HCT-116 Growth Inhibition Assay IC50=4.41007 μM SANGER
EPLC-272H Growth Inhibition Assay IC50=4.41533 μM SANGER
KS-1 Growth Inhibition Assay IC50=4.50889 μM SANGER
HT-1197 Growth Inhibition Assay IC50=4.52669 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=4.53686 μM SANGER
ES5 Growth Inhibition Assay IC50=4.83723 μM SANGER
CTB-1 Growth Inhibition Assay IC50=4.8488 μM SANGER
HL-60 Growth Inhibition Assay IC50=4.86611 μM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=4.86819 μM SANGER
MEG-01 Growth Inhibition Assay IC50=4.99403 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=5.20839 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=5.24043 μM SANGER
SW620 Growth Inhibition Assay IC50=5.24964 μM SANGER
U031 Growth Inhibition Assay IC50=5.25424 μM SANGER
TE-5 Growth Inhibition Assay IC50=5.4085 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=5.42472 μM SANGER
MG-63 Growth Inhibition Assay IC50=5.48762 μM SANGER
HC-1 Growth Inhibition Assay IC50=5.51839 μM SANGER
HCC2998 Growth Inhibition Assay IC50=5.52615 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=5.54537 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=5.60944 μM SANGER
D-423MG Growth Inhibition Assay IC50=5.61705 μM SANGER
SW962 Growth Inhibition Assay IC50=5.62032 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=5.63873 μM SANGER
LS-411N Growth Inhibition Assay IC50=5.79441 μM SANGER
NCI-H2291 Growth Inhibition Assay IC50=5.98943 μM SANGER
A549 Growth Inhibition Assay IC50=6.12553 μM SANGER
LS-1034 Growth Inhibition Assay IC50=6.20706 μM SANGER
NB14 Growth Inhibition Assay IC50=6.43836 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=6.63171 μM SANGER
BT-549 Growth Inhibition Assay IC50=6.66889 μM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=6.869 μM SANGER
SW756 Growth Inhibition Assay IC50=6.91176 μM SANGER
DJM-1 Growth Inhibition Assay IC50=6.92012 μM SANGER
GP5d Growth Inhibition Assay IC50=6.97394 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=7.02135 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=7.16405 μM SANGER
MN-60 Growth Inhibition Assay IC50=7.28089 μM SANGER
RMG-I Growth Inhibition Assay IC50=7.39296 μM SANGER
COLO-800 Growth Inhibition Assay IC50=7.41446 μM SANGER
DB Growth Inhibition Assay IC50=7.61005 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=7.64259 μM SANGER
HEL Growth Inhibition Assay IC50=7.71203 μM SANGER
NH-12 Growth Inhibition Assay IC50=7.72808 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=7.76771 μM SANGER
SW900 Growth Inhibition Assay IC50=7.82121 μM SANGER
JVM-3 Growth Inhibition Assay IC50=7.89599 μM SANGER
OAW-28 Growth Inhibition Assay IC50=7.94578 μM SANGER
KURAMOCHI Growth Inhibition Assay IC50=7.94811 μM SANGER
BE-13 Growth Inhibition Assay IC50=7.98112 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=8.01697 μM SANGER
NCI-H727 Growth Inhibition Assay IC50=8.1042 μM SANGER
SW1710 Growth Inhibition Assay IC50=8.18515 μM SANGER
D-502MG Growth Inhibition Assay IC50=8.29282 μM SANGER
NCI-H1993 Growth Inhibition Assay IC50=8.33631 μM SANGER
SCC-4 Growth Inhibition Assay IC50=8.44059 μM SANGER
HAL-01 Growth Inhibition Assay IC50=8.5191 μM SANGER
GT3TKB Growth Inhibition Assay IC50=8.67964 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=8.71329 μM SANGER
COLO-829 Growth Inhibition Assay IC50=8.80976 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=8.95481 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=9.0219 μM SANGER
BFTC-909 Growth Inhibition Assay IC50=9.06799 μM SANGER
EW-11 Growth Inhibition Assay IC50=9.17653 μM SANGER
HCE-4 Growth Inhibition Assay IC50=9.21558 μM SANGER
BALL-1 Growth Inhibition Assay IC50=9.21907 μM SANGER
SF539 Growth Inhibition Assay IC50=9.23562 μM SANGER
CAMA-1 Growth Inhibition Assay IC50=9.28128 μM SANGER
C32 Growth Inhibition Assay IC50=9.33064 μM SANGER
NCI-H1703 Growth Inhibition Assay IC50=9.34375 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=9.60946 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=9.76031 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=9.87383 μM SANGER
UM-UC-3 Growth Inhibition Assay IC50=9.9503 μM SANGER
BxPC-3 Growth Inhibition Assay IC50=10.0972 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=10.1999 μM SANGER
DEL Growth Inhibition Assay IC50=10.3946 μM SANGER
HuCCT1 Growth Inhibition Assay IC50=10.6033 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=10.8835 μM SANGER
CAL-72 Growth Inhibition Assay IC50=10.9391 μM SANGER
HCC1954 Growth Inhibition Assay IC50=11.0754 μM SANGER
EFO-21 Growth Inhibition Assay IC50=11.1045 μM SANGER
FTC-133 Growth Inhibition Assay IC50=11.1407 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=11.2366 μM SANGER
UACC-62 Growth Inhibition Assay IC50=11.2368 μM SANGER
NCI-H650 Growth Inhibition Assay IC50=11.2418 μM SANGER
ALL-PO Growth Inhibition Assay IC50=11.2512 μM SANGER
T84 Growth Inhibition Assay IC50=11.3907 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=11.4559 μM SANGER
SW626 Growth Inhibition Assay IC50=11.5755 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=11.5885 μM SANGER
MC-IXC Growth Inhibition Assay IC50=11.6728 μM SANGER
HOP-62 Growth Inhibition Assay IC50=11.6764 μM SANGER
NOS-1 Growth Inhibition Assay IC50=11.7109 μM SANGER
SW1573 Growth Inhibition Assay IC50=11.7295 μM SANGER
WM-115 Growth Inhibition Assay IC50=11.7588 μM SANGER
HuO9 Growth Inhibition Assay IC50=11.8774 μM SANGER
YAPC Growth Inhibition Assay IC50=11.9259 μM SANGER
MDA-MB-453 Growth Inhibition Assay IC50=11.9515 μM SANGER
NCI-H596 Growth Inhibition Assay IC50=12.0369 μM SANGER
A172 Growth Inhibition Assay IC50=12.0798 μM SANGER
RS4-11 Growth Inhibition Assay IC50=12.1725 μM SANGER
HCC1937 Growth Inhibition Assay IC50=12.7564 μM SANGER
SW837 Growth Inhibition Assay IC50=12.9028 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=12.9234 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=13.06 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=13.0632 μM SANGER
SK-UT-1 Growth Inhibition Assay IC50=13.1083 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=13.1593 μM SANGER
8505C Growth Inhibition Assay IC50=13.2067 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=13.7135 μM SANGER
LK-2 Growth Inhibition Assay IC50=13.7639 μM SANGER
OE33 Growth Inhibition Assay IC50=13.786 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=14.0202 μM SANGER
EW-13 Growth Inhibition Assay IC50=14.0352 μM SANGER
NCI-H1793 Growth Inhibition Assay IC50=14.2087 μM SANGER
BHT-101 Growth Inhibition Assay IC50=14.241 μM SANGER
RKO Growth Inhibition Assay IC50=14.5075 μM SANGER
NEC8 Growth Inhibition Assay IC50=14.5472 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=14.6247 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=14.6448 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=14.764 μM SANGER
EM-2 Growth Inhibition Assay IC50=14.8576 μM SANGER
HCC1395 Growth Inhibition Assay IC50=14.9338 μM SANGER
A2058 Growth Inhibition Assay IC50=15.0409 μM SANGER
SW1463 Growth Inhibition Assay IC50=15.0485 μM SANGER
J82 Growth Inhibition Assay IC50=15.057 μM SANGER
CAL-120 Growth Inhibition Assay IC50=15.1447 μM SANGER
COLO-824 Growth Inhibition Assay IC50=15.1579 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=15.4248 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=15.4688 μM SANGER
OC-314 Growth Inhibition Assay IC50=15.4714 μM SANGER
OVCAR-8 Growth Inhibition Assay IC50=15.8861 μM SANGER
MFE-280 Growth Inhibition Assay IC50=16.0488 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=16.0839 μM SANGER
SW1990 Growth Inhibition Assay IC50=16.1755 μM SANGER
U-266 Growth Inhibition Assay IC50=16.2299 μM SANGER
MFM-223 Growth Inhibition Assay IC50=16.3965 μM SANGER
L-363 Growth Inhibition Assay IC50=16.4577 μM SANGER
MCF7 Growth Inhibition Assay IC50=16.4723 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=16.4787 μM SANGER
HH Growth Inhibition Assay IC50=16.5162 μM SANGER
no-10 Growth Inhibition Assay IC50=16.6343 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=16.6576 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=16.7105 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=16.8316 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=16.8403 μM SANGER
ES3 Growth Inhibition Assay IC50=16.9134 μM SANGER
COLO-684 Growth Inhibition Assay IC50=16.9477 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=16.9694 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=17.0343 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=17.1974 μM SANGER
U-2-OS Growth Inhibition Assay IC50=17.5307 μM SANGER
RERF-LC-MS Growth Inhibition Assay IC50=17.5508 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=17.557 μM SANGER
ES8 Growth Inhibition Assay IC50=17.6087 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=17.8934 μM SANGER
RH-18 Growth Inhibition Assay IC50=18.0035 μM SANGER
D-283MED Growth Inhibition Assay IC50=18.0088 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=18.0559 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=18.1641 μM SANGER
SW982 Growth Inhibition Assay IC50=18.2671 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=18.4428 μM SANGER
A704 Growth Inhibition Assay IC50=18.4753 μM SANGER
ESS-1 Growth Inhibition Assay IC50=18.5205 μM SANGER
SCH Growth Inhibition Assay IC50=18.6456 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=18.746 μM SANGER
Mo-T Growth Inhibition Assay IC50=18.8204 μM SANGER
Saos-2 Growth Inhibition Assay IC50=19.1162 μM SANGER
SW684 Growth Inhibition Assay IC50=19.1326 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=19.2242 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=19.2607 μM SANGER
JAR Growth Inhibition Assay IC50=19.299 μM SANGER
SK-MEL-28 Growth Inhibition Assay IC50=19.3363 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=19.5468 μM SANGER
ES7 Growth Inhibition Assay IC50=19.6292 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=19.6471 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=19.7238 μM SANGER
KYSE-510 Growth Inhibition Assay IC50=19.8748 μM SANGER
ES1 Growth Inhibition Assay IC50=19.9213 μM SANGER
PC-3 Growth Inhibition Assay IC50=19.9604 μM SANGER
GCT Growth Inhibition Assay IC50=20.3026 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=20.3422 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=20.5463 μM SANGER
COLO-741 Growth Inhibition Assay IC50=20.66 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=20.6697 μM SANGER
HCC1187 Growth Inhibition Assay IC50=20.6734 μM SANGER
Becker Growth Inhibition Assay IC50=20.7201 μM SANGER
LU-134-A Growth Inhibition Assay IC50=21.1026 μM SANGER
MKN45 Growth Inhibition Assay IC50=21.1551 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=21.2729 μM SANGER
EW-24 Growth Inhibition Assay IC50=21.3945 μM SANGER
SK-N-AS Growth Inhibition Assay IC50=21.8276 μM SANGER
NCI-H2052 Growth Inhibition Assay IC50=21.8963 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=22.1419 μM SANGER
NB10 Growth Inhibition Assay IC50=22.2371 μM SANGER
CHP-212 Growth Inhibition Assay IC50=22.3222 μM SANGER
KM12 Growth Inhibition Assay IC50=22.356 μM SANGER
JEG-3 Growth Inhibition Assay IC50=22.378 μM SANGER
LN-405 Growth Inhibition Assay IC50=22.5913 μM SANGER
HCT-15 Growth Inhibition Assay IC50=22.7441 μM SANGER
MLMA Growth Inhibition Assay IC50=22.747 μM SANGER
GI-1 Growth Inhibition Assay IC50=22.7658 μM SANGER
RT-112 Growth Inhibition Assay IC50=22.8616 μM SANGER
MPP-89 Growth Inhibition Assay IC50=22.8661 μM SANGER
A3-KAW Growth Inhibition Assay IC50=23.1003 μM SANGER
KALS-1 Growth Inhibition Assay IC50=23.1414 μM SANGER
SF126 Growth Inhibition Assay IC50=23.6924 μM SANGER
SiHa Growth Inhibition Assay IC50=23.9327 μM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=23.9499 μM SANGER
Daoy Growth Inhibition Assay IC50=24.126 μM SANGER
COR-L23 Growth Inhibition Assay IC50=24.1767 μM SANGER
KG-1 Growth Inhibition Assay IC50=24.1928 μM SANGER
L-428 Growth Inhibition Assay IC50=24.5791 μM SANGER
NCI-H520 Growth Inhibition Assay IC50=24.8861 μM SANGER
COLO-792 Growth Inhibition Assay IC50=25.2732 μM SANGER
NB12 Growth Inhibition Assay IC50=25.2947 μM SANGER
GAK Growth Inhibition Assay IC50=25.2963 μM SANGER
SW780 Growth Inhibition Assay IC50=25.3264 μM SANGER
GB-1 Growth Inhibition Assay IC50=25.4069 μM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=25.4785 μM SANGER
NCI-H1651 Growth Inhibition Assay IC50=25.597 μM SANGER
KE-37 Growth Inhibition Assay IC50=25.7315 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=25.967 μM SANGER
SF295 Growth Inhibition Assay IC50=26.0425 μM SANGER
G-361 Growth Inhibition Assay IC50=26.1027 μM SANGER
HOP-92 Growth Inhibition Assay IC50=26.1226 μM SANGER
UMC-11 Growth Inhibition Assay IC50=26.4514 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=26.6591 μM SANGER
TE-11 Growth Inhibition Assay IC50=26.7752 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=26.9108 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=27.0176 μM SANGER
BCPAP Growth Inhibition Assay IC50=27.137 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=27.2561 μM SANGER
EW-16 Growth Inhibition Assay IC50=27.2947 μM SANGER
HT-144 Growth Inhibition Assay IC50=27.4032 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=27.4447 μM SANGER
T98G Growth Inhibition Assay IC50=27.5846 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=27.7562 μM SANGER
BEN Growth Inhibition Assay IC50=27.8517 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=28.2795 μM SANGER
HuH-7 Growth Inhibition Assay IC50=28.4028 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=28.433 μM SANGER
AN3-CA Growth Inhibition Assay IC50=28.4395 μM SANGER
EGI-1 Growth Inhibition Assay IC50=28.5928 μM SANGER
697 Growth Inhibition Assay IC50=28.6331 μM SANGER
TCCSUP Growth Inhibition Assay IC50=28.6418 μM SANGER
GR-ST Growth Inhibition Assay IC50=28.6696 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=28.6885 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=28.7959 μM SANGER
IGR-1 Growth Inhibition Assay IC50=28.8874 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=29.2705 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=29.3145 μM SANGER
RD Growth Inhibition Assay IC50=29.5233 μM SANGER
SF268 Growth Inhibition Assay IC50=29.5931 μM SANGER
SHP-77 Growth Inhibition Assay IC50=29.6182 μM SANGER
D-566MG Growth Inhibition Assay IC50=29.9393 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=30.1238 μM SANGER
MEL-HO Growth Inhibition Assay IC50=30.1423 μM SANGER
SJRH30 Growth Inhibition Assay IC50=30.2108 μM SANGER
D-336MG Growth Inhibition Assay IC50=30.2892 μM SANGER
C3A Growth Inhibition Assay IC50=30.2927 μM SANGER
Calu-6 Growth Inhibition Assay IC50=30.2963 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=30.393 μM SANGER
KYSE-70 Growth Inhibition Assay IC50=30.5114 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=30.5181 μM SANGER
DK-MG Growth Inhibition Assay IC50=30.5456 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=30.6326 μM SANGER
MS-1 Growth Inhibition Assay IC50=30.8889 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=31.0571 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=31.4006 μM SANGER
NB17 Growth Inhibition Assay IC50=31.5185 μM SANGER
639-V Growth Inhibition Assay IC50=31.5243 μM SANGER
CAL-51 Growth Inhibition Assay IC50=31.5667 μM SANGER
HGC-27 Growth Inhibition Assay IC50=31.5873 μM SANGER
GOTO Growth Inhibition Assay IC50=31.8506 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=32.007 μM SANGER
RO82-W-1 Growth Inhibition Assay IC50=32.1604 μM SANGER
SH-4 Growth Inhibition Assay IC50=32.1858 μM SANGER
A204 Growth Inhibition Assay IC50=32.5069 μM SANGER
DMS-273 Growth Inhibition Assay IC50=32.5322 μM SANGER
KGN Growth Inhibition Assay IC50=32.633 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=32.6527 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=32.6602 μM SANGER
MKN28 Growth Inhibition Assay IC50=32.7838 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=32.9678 μM SANGER
ATN-1 Growth Inhibition Assay IC50=33.1416 μM SANGER
D-263MG Growth Inhibition Assay IC50=33.8378 μM SANGER
LU-135 Growth Inhibition Assay IC50=33.8829 μM SANGER
C8166 Growth Inhibition Assay IC50=33.8854 μM SANGER
T-24 Growth Inhibition Assay IC50=34.0205 μM SANGER
Mewo Growth Inhibition Assay IC50=34.1349 μM SANGER
22RV1 Growth Inhibition Assay IC50=34.1754 μM SANGER
KM-H2 Growth Inhibition Assay IC50=34.1779 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=34.3471 μM SANGER
ABC-1 Growth Inhibition Assay IC50=34.3693 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=34.3889 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=34.5703 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=34.6487 μM SANGER
NCI-H810 Growth Inhibition Assay IC50=34.7278 μM SANGER
D-392MG Growth Inhibition Assay IC50=35.0565 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=35.1658 μM SANGER
COLO-679 Growth Inhibition Assay IC50=35.388 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=35.4369 μM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=35.4649 μM SANGER
KNS-42 Growth Inhibition Assay IC50=35.5826 μM SANGER
RVH-421 Growth Inhibition Assay IC50=35.7645 μM SANGER
P30-OHK Growth Inhibition Assay IC50=35.8752 μM SANGER
G-402 Growth Inhibition Assay IC50=35.9867 μM SANGER
S-117 Growth Inhibition Assay IC50=36.3008 μM SANGER
RXF393 Growth Inhibition Assay IC50=36.3785 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=36.7803 μM SANGER
U-118-MG Growth Inhibition Assay IC50=36.8847 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=36.9483 μM SANGER
MFH-ino Growth Inhibition Assay IC50=37.3371 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=37.4196 μM SANGER
NCI-H446 Growth Inhibition Assay IC50=37.4862 μM SANGER
LU-99A Growth Inhibition Assay IC50=37.5731 μM SANGER
KP-N-YN Growth Inhibition Assay IC50=37.6195 μM SANGER
SCC-9 Growth Inhibition Assay IC50=37.7838 μM SANGER
EFM-19 Growth Inhibition Assay IC50=37.7967 μM SANGER
A427 Growth Inhibition Assay IC50=37.9107 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=38.6039 μM SANGER
HOS Growth Inhibition Assay IC50=39.6273 μM SANGER
LAN-6 Growth Inhibition Assay IC50=40.0112 μM SANGER
U251 Growth Inhibition Assay IC50=40.4054 μM SANGER
SNU-387 Growth Inhibition Assay IC50=40.4553 μM SANGER
DMS-79 Growth Inhibition Assay IC50=40.5889 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=40.6568 μM SANGER
HT Growth Inhibition Assay IC50=40.6639 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=40.6768 μM SANGER
DMS-114 Growth Inhibition Assay IC50=40.8374 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=41.0569 μM SANGER
ONS-76 Growth Inhibition Assay IC50=41.4709 μM SANGER
A673 Growth Inhibition Assay IC50=41.5157 μM SANGER
HPAF-II Growth Inhibition Assay IC50=41.6709 μM SANGER
UACC-257 Growth Inhibition Assay IC50=41.7369 μM SANGER
EW-22 Growth Inhibition Assay IC50=41.8697 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=41.8725 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=42.1782 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=42.4955 μM SANGER
NB13 Growth Inhibition Assay IC50=42.6217 μM SANGER
SW872 Growth Inhibition Assay IC50=42.6331 μM SANGER
KP-4 Growth Inhibition Assay IC50=42.8832 μM SANGER
HCC38 Growth Inhibition Assay IC50=42.9618 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=43.2356 μM SANGER
CAL-62 Growth Inhibition Assay IC50=43.4028 μM SANGER
NCI-H2029 Growth Inhibition Assay IC50=43.5581 μM SANGER
M14 Growth Inhibition Assay IC50=44.1332 μM SANGER
COLO-680N Growth Inhibition Assay IC50=44.339 μM SANGER
Hs-578-T Growth Inhibition Assay IC50=45.0294 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=45.9482 μM SANGER
EW-1 Growth Inhibition Assay IC50=45.9689 μM SANGER
SW948 Growth Inhibition Assay IC50=46.4462 μM SANGER
NCI-H460 Growth Inhibition Assay IC50=46.523 μM SANGER
CAS-1 Growth Inhibition Assay IC50=46.7701 μM SANGER
TGBC11TKB Growth Inhibition Assay IC50=47.1777 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=48.786 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=49.7785 μM SANGER
PA-1 Growth Inhibition Assay IC50=49.8335 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=49.8723 μM SANGER
A101D Growth Inhibition Assay IC50=49.9425 μM SANGER
NCI-H2087 Growth Inhibition Assay IC50=49.9682 μM SANGER

... Click to View More Cell Line Experimental Data

In vivo Daily oral administration of BIBW2992 at 20 mg/kg for 25 days results in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%. Reduced phosphorylation of EGFR and AKT is confirmed by immunohistochemical staining of tissue sections. Therefore, like lapatinib and neratinib, BIBW2992 is a next generation tyrosine kinase inhibitor (TKI) that inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases irreversibly. BIBW2992 is not only active against EGFR mutations targeted by first generation TKIs like Erlotinib or Gefitinib, but also against those insensitive to these standard therapies. [1]