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Afatinib
Synonyms: BIBW2992
Afatinib inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.
Afatinib Chemical Structure
CAS No. 850140-72-6
Purity & Quality Control
Batch:
Purity:
99.95%
99.95
Afatinib Related Products
Signaling Pathway
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 | ||||||
Biological Activity
| Description | Afatinib inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy. | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Targets |
|
| In vitro | ||||
| 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] | |||
|---|---|---|---|---|
| Kinase Assay | In vitro kinase activity assays | |||
| The wild type tyrosine kinase domain of the human EGFR as well as that of the EGFR L858R/T790M double mutant are fused to Glutathione-S-transferase (GST), and extracted. Enzyme activity is then assayed in the presence of the inhibitor BIBW2992, serially diluted in 50% DMSO. A random polymer pEY (4:1) is used as substrate and biotinylated pEY (bio-pEY) is added as a tracer substrate. The kinase domain of HER2 is cloned using the baculovirus system and extracted similarly to that of EGFR kinase. Details of assays for EGFR, HER2, SRC, BIRK and VEGFR2 kinase activity are available in Supplementary information. | ||||
| Cell Research | Cell lines | NSCLC cells | ||
| Concentrations | 0-10 μM | |||
| Incubation Time | 1 hour | |||
| Method | 1 × 104 NSCLC cells are transferred into each well of a 96-well plate and cultured overnight in serum-free media for the EGFR phosphorylation assay. After addition of BIBW2992 on the next day, the plates are incubated at 37 °C for 1 hour. EGF-stimulation is done using 100 ng/mL for 10 min at room temperature. Cells are washed with ice cold PBS, extracted with 120 μL HEPEX buffer per well and shaken at room temperature for 1 hour. In all 2 × 104 cells per well is used for the HER2 phosphorylation assay. Streptavidin precoated plates are coated with anti-EGFR-biotin at 1:100 dilution in blocking buffer and c-erb2/HER2 oncoprotein Ab-5(Clone N24)-Biotin. Cell extracts is then transferred to the antibody-coated wells and incubated at room temperature for 1 hour. Extinction is measured at 450 nm. |
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| Experimental Result Images | Methods | Biomarkers | Images | PMID |
| Western blot | CIP2A / p-AKT / AKT / PARP p-EGFR / p-IGF1R / p-ERK / p-AKT p-VEGFR2 / VEGFR2 / JAG1 / DLL4 / NICD1 |
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25537503 | |
| Growth inhibition assay | Cell apoptosis Cell viability |
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25537503 | |
| Immunofluorescence | p65 vacuoles |
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26317651 | |
| In Vivo | ||
| 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] | |
|---|---|---|
| Animal Research | Animal Models | Athymic NMRI-nu/nu female mice |
| Dosages | 20 mg/kg | |
| Administration | Oral administration | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06302621 | Recruiting | Advanced Solid Tumor|Unresectable Solid Tumor|Metastatic Solid Tumor|Cholangiocarcinoma |
Massachusetts General Hospital|Boehringer Ingelheim|Incyte Corporation |
July 1 2024 | Phase 1 |
| NCT05298176 | Recruiting | Non-Small Cell Lung Cancer |
Amsterdam UMC location VUmc |
January 4 2022 | Phase 2 |
| NCT04795245 | Completed | Non-squamous Non-Small Cell Lung Cancer |
Boehringer Ingelheim |
August 26 2021 | -- |
| NCT04497584 | Recruiting | Advanced Squamous Non Small Cell Lung Cancer |
University of Texas Southwestern Medical Center |
August 4 2021 | Phase 2 |
| NCT04413201 | Active not recruiting | Non-squamous NSCLC |
Michael Hopp|Boehringer Ingelheim|Johannes Gutenberg University Mainz |
September 11 2020 | Phase 4 |
Chemical Information & Solubility
| Molecular Weight | 485.94 | Formula | C24H25ClFN5O3 |
| CAS No. | 850140-72-6 | SDF | Download Afatinib SDF |
| Smiles | CN(C)CC=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OC4CCOC4 | ||
| Storage (From the date of receipt) | |||
|
In vitro |
DMSO : 97 mg/mL ( (199.61 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.) Ethanol : 97 mg/mL Water : Insoluble |
Molecular Weight Calculator |
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In vivo Add solvents to the product individually and in order. |
In vivo Formulation Calculator |
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Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
Question 1:
What’s the recommendation about reconstitution of the compound for in vivo animal study?
Answer:
For in vivo experiment of afatinib, we recommend 0.5% methylcellulose/0.2% Tween 80 as vehicle.
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