Afatinib
别名: BIBW2992 中文名称：阿法替尼
Afatinib不可逆地抑制EGFR/ErbB，包括EGFR(wt)，EGFR(L858R)，EGFR(L858R/T790M)，ErbB2（HER2）和ErbB4（HER4），在无细胞试验中IC50分别为0.5 nM，0.4 nM，10 nM，14 nM和1 nM。Afatinib可诱导自噬。
Afatinib Chemical Structure
CAS: 850140-72-6
产品质控
批次：
纯度：
99.98%
99.98
Afatinib相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| NCI-H1299 | Growth Inhibition Assay | IC50=6.63171 μM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=6.43836 μM | SANGER | ||
| LS-1034 | Growth Inhibition Assay | IC50=6.20706 μM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=6.12553 μM | SANGER | ||
| NCI-H2291 | Growth Inhibition Assay | IC50=5.98943 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=5.79441 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=5.63873 μM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=5.62032 μM | SANGER | ||
| D-423MG | Growth Inhibition Assay | IC50=5.61705 μM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=5.60944 μM | SANGER | ||
| NTERA-S-cl-D1 | Growth Inhibition Assay | IC50=5.54537 μM | SANGER | ||
| HCC2998 | Growth Inhibition Assay | IC50=5.52615 μM | SANGER | ||
| HC-1 | Growth Inhibition Assay | IC50=5.51839 μM | SANGER | ||
| MG-63 | Growth Inhibition Assay | IC50=5.48762 μM | SANGER | ||
| NCI-H747 | Growth Inhibition Assay | IC50=5.42472 μM | SANGER | ||
| TE-5 | Growth Inhibition Assay | IC50=5.4085 μM | SANGER | ||
| U031 | Growth Inhibition Assay | IC50=5.25424 μM | SANGER | ||
| SW620 | Growth Inhibition Assay | IC50=5.24964 μM | SANGER | ||
| HuO-3N1 | Growth Inhibition Assay | IC50=5.24043 μM | SANGER | ||
| KYSE-520 | Growth Inhibition Assay | IC50=5.20839 μM | SANGER | ||
| MEG-01 | Growth Inhibition Assay | IC50=4.99403 μM | SANGER | ||
| VM-CUB-1 | Growth Inhibition Assay | IC50=4.86819 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=4.86611 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=4.8488 μM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=4.83723 μM | SANGER | ||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=4.53686 μM | SANGER | ||
| HT-1197 | Growth Inhibition Assay | IC50=4.52669 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=4.50889 μM | SANGER | ||
| EPLC-272H | Growth Inhibition Assay | IC50=4.41533 μM | SANGER | ||
| HCT-116 | Growth Inhibition Assay | IC50=4.41007 μM | SANGER | ||
| KLE | Growth Inhibition Assay | IC50=4.40819 μM | SANGER | ||
| LS-513 | Growth Inhibition Assay | IC50=4.31217 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=4.1702 μM | SANGER | ||
| SW1417 | Growth Inhibition Assay | IC50=4.12147 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=4.11631 μM | SANGER | ||
| U-87-MG | Growth Inhibition Assay | IC50=4.10481 μM | SANGER | ||
| 647-V | Growth Inhibition Assay | IC50=3.98452 μM | SANGER | ||
| MC116 | Growth Inhibition Assay | IC50=3.95489 μM | SANGER | ||
| KNS-62 | Growth Inhibition Assay | IC50=3.94731 μM | SANGER | ||
| GAMG | Growth Inhibition Assay | IC50=3.91314 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=3.87994 μM | SANGER | ||
| TE-9 | Growth Inhibition Assay | IC50=3.84382 μM | SANGER | ||
| NCI-H1693 | Growth Inhibition Assay | IC50=3.84181 μM | SANGER | ||
| KOSC-2 | Growth Inhibition Assay | IC50=3.83451 μM | SANGER | ||
| OCUB-M | Growth Inhibition Assay | IC50=3.76187 μM | SANGER | ||
| 8305C | Growth Inhibition Assay | IC50=3.75911 μM | SANGER | ||
| LS-123 | Growth Inhibition Assay | IC50=3.74284 μM | SANGER | ||
| BT-20 | Growth Inhibition Assay | IC50=3.69795 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=3.69735 μM | SANGER | ||
| SNU-449 | Growth Inhibition Assay | IC50=3.65826 μM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=3.62217 μM | SANGER | ||
| NCI-H2009 | Growth Inhibition Assay | IC50=3.61216 μM | SANGER | ||
| NCI-H441 | Growth Inhibition Assay | IC50=3.59841 μM | SANGER | ||
| HEC-1 | Growth Inhibition Assay | IC50=3.5895 μM | SANGER | ||
| NY | Growth Inhibition Assay | IC50=3.53655 μM | SANGER | ||
| no-11 | Growth Inhibition Assay | IC50=3.53564 μM | SANGER | ||
| SKG-IIIa | Growth Inhibition Assay | IC50=3.52237 μM | SANGER | ||
| OAW-42 | Growth Inhibition Assay | IC50=3.50026 μM | SANGER | ||
| MKN1 | Growth Inhibition Assay | IC50=3.47108 μM | SANGER | ||
| Capan-2 | Growth Inhibition Assay | IC50=3.46875 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=3.18744 μM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=3.18254 μM | SANGER | ||
| RPMI-7951 | Growth Inhibition Assay | IC50=3.0759 μM | SANGER | ||
| HT-29 | Growth Inhibition Assay | IC50=3.07309 μM | SANGER | ||
| 786-0 | Growth Inhibition Assay | IC50=3.06408 μM | SANGER | ||
| SN12C | Growth Inhibition Assay | IC50=2.91964 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=2.74888 μM | SANGER | ||
| SNU-C2B | Growth Inhibition Assay | IC50=2.68616 μM | SANGER | ||
| TE-10 | Growth Inhibition Assay | IC50=2.68078 μM | SANGER | ||
| OVCAR-3 | Growth Inhibition Assay | IC50=2.67167 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=2.63565 μM | SANGER | ||
| HCC1569 | Growth Inhibition Assay | IC50=2.58297 μM | SANGER | ||
| HT55 | Growth Inhibition Assay | IC50=2.5738 μM | SANGER | ||
| RCM-1 | Growth Inhibition Assay | IC50=2.52938 μM | SANGER | ||
| NCI-H1048 | Growth Inhibition Assay | IC50=2.49158 μM | SANGER | ||
| MKN7 | Growth Inhibition Assay | IC50=2.35335 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=2.29676 μM | SANGER | ||
| 769-P | Growth Inhibition Assay | IC50=2.29037 μM | SANGER | ||
| CaR-1 | Growth Inhibition Assay | IC50=2.28281 μM | SANGER | ||
| MDA-MB-157 | Growth Inhibition Assay | IC50=2.21828 μM | SANGER | ||
| PANC-03-27 | Growth Inhibition Assay | IC50=2.16631 μM | SANGER | ||
| LoVo | Growth Inhibition Assay | IC50=2.10797 μM | SANGER | ||
| OMC-1 | Growth Inhibition Assay | IC50=2.08169 μM | SANGER | ||
| A2780 | Growth Inhibition Assay | IC50=2.06294 μM | SANGER | ||
| GMS-10 | Growth Inhibition Assay | IC50=2.03517 μM | SANGER | ||
| KYSE-270 | Growth Inhibition Assay | IC50=2.02732 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=1.91377 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=1.88945 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=1.81475 μM | SANGER | ||
| NCI-H1666 | Growth Inhibition Assay | IC50=1.80948 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=1.80414 μM | SANGER | ||
| CAKI-1 | Growth Inhibition Assay | IC50=1.78211 μM | SANGER | ||
| OE19 | Growth Inhibition Assay | IC50=1.71512 μM | SANGER | ||
| Detroit562 | Growth Inhibition Assay | IC50=1.70152 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=1.6823 μM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=1.67413 μM | SANGER | ||
| KYSE-410 | Growth Inhibition Assay | IC50=1.65672 μM | SANGER | ||
| ME-180 | Growth Inhibition Assay | IC50=1.61096 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=1.58357 μM | SANGER | ||
| ECC10 | Growth Inhibition Assay | IC50=1.55369 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=1.54006 μM | SANGER | ||
| NCI-H630 | Growth Inhibition Assay | IC50=1.45582 μM | SANGER | ||
| CFPAC-1 | Growth Inhibition Assay | IC50=1.42493 μM | SANGER | ||
| NB5 | Growth Inhibition Assay | IC50=1.41317 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=1.40121 μM | SANGER | ||
| SCC-15 | Growth Inhibition Assay | IC50=1.39451 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=1.37456 μM | SANGER | ||
| HT-3 | Growth Inhibition Assay | IC50=1.28753 μM | SANGER | ||
| SW48 | Growth Inhibition Assay | IC50=1.25432 μM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=1.239 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=1.20214 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=1.17513 μM | SANGER | ||
| PANC-08-13 | Growth Inhibition Assay | IC50=1.16416 μM | SANGER | ||
| SK-MES-1 | Growth Inhibition Assay | IC50=1.11487 μM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=1.08104 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=1.07883 μM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=1.05419 μM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=1.02945 μM | SANGER | ||
| HT-1376 | Growth Inhibition Assay | IC50=1.01513 μM | SANGER | ||
| 5637 | Growth Inhibition Assay | IC50=1.0151 μM | SANGER | ||
| SW1116 | Growth Inhibition Assay | IC50=1.01287 μM | SANGER | ||
| D-542MG | Growth Inhibition Assay | IC50=1.01064 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=1.01064 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=0.97836 μM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=0.88428 μM | SANGER | ||
| JVM-2 | Growth Inhibition Assay | IC50=0.88299 μM | SANGER | ||
| SCC-25 | Growth Inhibition Assay | IC50=0.84171 μM | SANGER | ||
| AGS | Growth Inhibition Assay | IC50=0.83648 μM | SANGER | ||
| Calu-3 | Growth Inhibition Assay | IC50=0.81434 μM | SANGER | ||
| C-33-A | Growth Inhibition Assay | IC50=0.81297 μM | SANGER | ||
| COLO-678 | Growth Inhibition Assay | IC50=0.80834 μM | SANGER | ||
| KU-19-19 | Growth Inhibition Assay | IC50=0.77464 μM | SANGER | ||
| NCI-H1573 | Growth Inhibition Assay | IC50=0.7363 μM | SANGER | ||
| MDA-MB-361 | Growth Inhibition Assay | IC50=0.72662 μM | SANGER | ||
| HuP-T4 | Growth Inhibition Assay | IC50=0.6976 μM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=0.69666 μM | SANGER | ||
| EW-18 | Growth Inhibition Assay | IC50=0.68698 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=0.64392 μM | SANGER | ||
| COR-L88 | Growth Inhibition Assay | IC50=0.64113 μM | SANGER | ||
| NCI-H1975 | Growth Inhibition Assay | IC50=0.61728 μM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=0.61621 μM | SANGER | ||
| NCI-H1838 | Growth Inhibition Assay | IC50=0.60299 μM | SANGER | ||
| HCC70 | Growth Inhibition Assay | IC50=0.57661 μM | SANGER | ||
| ACN | Growth Inhibition Assay | IC50=0.55094 μM | SANGER | ||
| FADU | Growth Inhibition Assay | IC50=0.54404 μM | SANGER | ||
| NCI-H358 | Growth Inhibition Assay | IC50=0.5321 μM | SANGER | ||
| NCI-H2126 | Growth Inhibition Assay | IC50=0.51926 μM | SANGER | ||
| SAS | Growth Inhibition Assay | IC50=0.48398 μM | SANGER | ||
| A431 | Growth Inhibition Assay | IC50=0.48233 μM | SANGER | ||
| CW-2 | Growth Inhibition Assay | IC50=0.46914 μM | SANGER | ||
| DU-145 | Growth Inhibition Assay | IC50=0.44833 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=0.44182 μM | SANGER | ||
| A498 | Growth Inhibition Assay | IC50=0.40674 μM | SANGER | ||
| TE-6 | Growth Inhibition Assay | IC50=0.40246 μM | SANGER | ||
| KYSE-180 | Growth Inhibition Assay | IC50=0.39089 μM | SANGER | ||
| NUGC-3 | Growth Inhibition Assay | IC50=0.38373 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=0.36857 μM | SANGER | ||
| HCC1419 | Growth Inhibition Assay | IC50=0.36408 μM | SANGER | ||
| HLE | Growth Inhibition Assay | IC50=0.35046 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=0.34593 μM | SANGER | ||
| DoTc2-4510 | Growth Inhibition Assay | IC50=0.32219 μM | SANGER | ||
| ACHN | Growth Inhibition Assay | IC50=0.31994 μM | SANGER | ||
| 23132-87 | Growth Inhibition Assay | IC50=0.31923 μM | SANGER | ||
| LU-139 | Growth Inhibition Assay | IC50=0.3051 μM | SANGER | ||
| BHY | Growth Inhibition Assay | IC50=0.28655 μM | SANGER | ||
| HO-1-N-1 | Growth Inhibition Assay | IC50=0.27853 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.26892 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=0.26738 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=0.25952 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=0.24802 μM | SANGER | ||
| MOLT-13 | Growth Inhibition Assay | IC50=0.23975 μM | SANGER | ||
| NCI-H69 | Growth Inhibition Assay | IC50=0.21451 μM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=0.21198 μM | SANGER | ||
| COR-L105 | Growth Inhibition Assay | IC50=0.21084 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=0.2046 μM | SANGER | ||
| CAL-33 | Growth Inhibition Assay | IC50=0.20184 μM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=0.18959 μM | SANGER | ||
| CAL-27 | Growth Inhibition Assay | IC50=0.17636 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=0.17596 μM | SANGER | ||
| HSC-2 | Growth Inhibition Assay | IC50=0.16837 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=0.16576 μM | SANGER | ||
| SW13 | Growth Inhibition Assay | IC50=0.16216 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=0.15456 μM | SANGER | ||
| TI-73 | Growth Inhibition Assay | IC50=0.14715 μM | SANGER | ||
| HN | Growth Inhibition Assay | IC50=0.13077 μM | SANGER | ||
| LU-65 | Growth Inhibition Assay | IC50=0.12633 μM | SANGER | ||
| UACC-893 | Growth Inhibition Assay | IC50=0.11885 μM | SANGER | ||
| CAL-39 | Growth Inhibition Assay | IC50=0.11792 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=0.10884 μM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=0.1028 μM | SANGER | ||
| ZR-75-30 | Growth Inhibition Assay | IC50=0.09545 μM | SANGER | ||
| AU565 | Growth Inhibition Assay | IC50=0.08504 μM | SANGER | ||
| Ca9-22 | Growth Inhibition Assay | IC50=0.08353 μM | SANGER | ||
| KYSE-140 | Growth Inhibition Assay | IC50=0.0833 μM | SANGER | ||
| NCI-H1623 | Growth Inhibition Assay | IC50=0.08025 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=0.07823 μM | SANGER | ||
| H9 | Growth Inhibition Assay | IC50=0.07132 μM | SANGER | ||
| NCI-H292 | Growth Inhibition Assay | IC50=0.0609 μM | SANGER | ||
| BPH-1 | Growth Inhibition Assay | IC50=0.05988 μM | SANGER | ||
| KYSE-450 | Growth Inhibition Assay | IC50=0.05978 μM | SANGER | ||
| EC-GI-10 | Growth Inhibition Assay | IC50=0.05912 μM | SANGER | ||
| PC-14 | Growth Inhibition Assay | IC50=0.05668 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=0.05325 μM | SANGER | ||
| EFO-27 | Growth Inhibition Assay | IC50=0.05182 μM | SANGER | ||
| BT-474 | Growth Inhibition Assay | IC50=0.04986 μM | SANGER | ||
| NCI-H2170 | Growth Inhibition Assay | IC50=0.03728 μM | SANGER | ||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=0.03416 μM | SANGER | ||
| DSH1 | Growth Inhibition Assay | IC50=0.03314 μM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=0.03194 μM | SANGER | ||
| NCI-N87 | Growth Inhibition Assay | IC50=0.02773 μM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=0.0206 μM | SANGER | ||
| CHL-1 | Growth Inhibition Assay | IC50=0.01839 μM | SANGER | ||
| HSC-4 | Growth Inhibition Assay | IC50=0.01748 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=0.01671 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=0.00987 μM | SANGER | ||
| KASUMI-1 | Growth Inhibition Assay | IC50=0.00911 μM | SANGER | ||
| HDLM-2 | Growth Inhibition Assay | IC50=0.00572 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Afatinib不可逆地抑制EGFR/ErbB，包括EGFR(wt)，EGFR(L858R)，EGFR(L858R/T790M)，ErbB2（HER2）和ErbB4（HER4），在无细胞试验中IC50分别为0.5 nM，0.4 nM，10 nM，14 nM和1 nM。Afatinib可诱导自噬。 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | BIBW2992不可逆地抑制EGFR/HER2，在体外作用于野生型EGFR ,L858R突变型EGFR, L858R/T790M 双突变型EGFR，及HER2时IC50分别为0.5, 0.4, 10, 14 nM。在体外实验中，BIBW2992不管作用于野生型EGFR/HER2还是突变型EGFR/HER2都显示出强大的活力，与gefitinib作用于L858R突变型EGFR的活力差不多，但是要比gefitinib 作用于L858R-T790M双突变型EGFR的活力大100倍。在体外，BIBW2992有效抑制所有实验类型细胞的EGFR/HER磷酸化作用。比如人类扁平上皮癌A431细胞系表达的野生型EGFR, 鼠类NIH-3T3细胞转染的野生型HER2 , 以及乳腺癌BT-474细胞系和胃癌NCI-N87细胞系表达的内源性HER2。[1] | |||
|---|---|---|---|---|
| 激酶实验 | 体外激酶活性实验 | |||
| 人类EGFR和L858R/T790M双重突变型EGFR 的酪氨酸激酶区域与谷胱甘肽巯基转移酶区域相接，提取酪氨酸激酶区域的方法见补充说明。在有和没有BIBW2992时分别测定酶活。使用杆状病毒系统克隆HER2激酶，用类似提取EGFR激酶域的方法提取HER2激酶域。 | ||||
| 细胞实验 | 细胞系 | NSCLC细胞 | ||
| 浓度 | 0-10 μM | |||
| 孵育时间 | 1小时 | |||
| 方法 | 细胞按1×104密度转移到96孔板上，在无血清培养基上过夜培养，用于EGFR磷酸化实验。第二天添加包含BIBW2992的混合物，培养基在37oC温育1小时。在室温下用100 ng/ml EGF刺激10分钟。细胞用冰冻PBS冲洗，然后每孔用120 μl HEPEX buffer萃取，然后在室温下震荡1小时。每孔中所有2×104细胞都用于HER2磷酸化实验。在涂有链霉亲和素的板上加用封闭液按1:100比例稀释的抗EGFR的生物素和c-erb2/HER2肿瘤蛋白Ab-5-生物素。上述步骤得到的萃取物转移到有抗体包被的孔中，室温下温育1小时。彩色显影的测法见补充说明，吸光度为450纳米。 |
|||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-EGFR / p-IGF1R / p-ERK / p-AKT CIP2A / p-AKT / AKT / PARP p-VEGFR2 / VEGFR2 / JAG1 / DLL4 / NICD1 |
|
26052929 | |
| Growth inhibition assay | Cell viability Cell apoptosis |
|
26515464 | |
| Immunofluorescence | vacuoles p65 |
|
29713246 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 活体研究时按实验对象体重，每千克口服20 mg BIBW2992持续25天，肿瘤产生明显的衰退现象，通过肿瘤切片的免疫组织化学染色观察发现，EGFR和AKT的磷酸化作用收到抑制。因此，正如lapatinib和neratinib, BIBW2992是次代酪氨酸激酶抑制剂，不可逆地抑制人类EGFR2（HER2）和EGFR激酶。BIBW2992不仅能和原代酪氨酸激酶如erlotinib和gefitinib一样有效抑制EGFR突变型，而且还能作用于抗erlotinib和gefitinib的EGFR。[1] | |
|---|---|---|
| 动物实验 | Animal Models | 雌性无胸腺NMRI-nu/nu鼠 |
| Dosages | 20 mg/kg | |
| Administration | 口服处理 | |
| 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 |
化学信息&溶解度
| 分子量 | 485.94 | 分子式 | C24H25ClFN5O3 |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 97 mg/mL ( (199.61 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 87 mg/mL (179.03 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
What’s the recommendation about reconstitution of the compound for in vivo animal study?
回答：
For in vivo experiment of afatinib, we recommend 0.5% methylcellulose/0.2% Tween 80 as vehicle.
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