Dabrafenib
别名: GSK2118436, GSK2118436A 中文名称：达拉菲尼,达拉非尼
Dabrafenib是一种突变型BRAFV600E特异性抑制剂，无细胞试验中IC50为0.7 nM，作用于B-Raf(wt)和c-Raf效果分别低7和9倍。
Dabrafenib Chemical Structure
CAS: 1195765-45-7
产品质控
批次：
纯度：
99.99%
99.99
Dabrafenib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 |
|---|---|---|---|---|---|
| HuNS-1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| IGROV1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| HT-3 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| HT | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| HPAF-II | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| Hs746.T | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| HOS | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| HN5 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| HMCB | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| Hep3B | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| Hela | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| HCC-1954 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| HCC-70 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| G401 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| FaDu | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| EKVX | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| EFM-19 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| EB-3 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| DU-145 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| DOTC 24510 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| Daudi | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| CRO-AP2 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| COR-L23 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| Colo704 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| Colo320DM | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| CHL-1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| CGTHW1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| CaOV3 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| Calu-3 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| CAL-62 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| CAL-27 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| C33A | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| C-4 I | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| BxPc3 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| BT-20 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| Be(2)C | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| ARH-77 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| A2780 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| A431 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| A427 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| A204 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| A172 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| 786-O | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| 647-V | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| 22Rv1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| MES-SA | Growth Inhibition Assay | 10 μM | 72 h | IC50=6.989 μM | 23844038 |
| C3A | Growth Inhibition Assay | 10 μM | 72 h | IC50=5.414 μM | 23844038 |
| HL-60 | Growth Inhibition Assay | 10 μM | 72 h | IC50=2.178 μM | 23844038 |
| HT-1080 | Growth Inhibition Assay | 10 μM | 72 h | IC50=2.004 μM | 23844038 |
| GDM-1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=1.997 μM | 23844038 |
| CEM/C1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=1.773 μM | 23844038 |
| SNU-1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=1.501 μM | 23844038 |
| MC/CAR | Growth Inhibition Assay | 10 μM | 72 h | IC50=1.002 μM | 23844038 |
| RPMI-6666 | Growth Inhibition Assay | 10 μM | 72 h | IC50=928 nM | 23844038 |
| DB | Growth Inhibition Assay | 10 μM | 72 h | IC50=873 nM | 23844038 |
| BC-1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=704 nM | 23844038 |
| H4 | Growth Inhibition Assay | 10 μM | 72 h | IC50=619 nM | 23844038 |
| CESS | Growth Inhibition Assay | 10 μM | 72 h | IC50=497 nM | 23844038 |
| SK-MES-1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=329 nM | 23844038 |
| JRT3-T35 | Growth Inhibition Assay | 10 μM | 72 h | IC50=295 nM | 23844038 |
| ACHN | Growth Inhibition Assay | 10 μM | 72 h | IC50=294 nM | 23844038 |
| BC-3 | Growth Inhibition Assay | 10 μM | 72 h | IC50=277 nM | 23844038 |
| RPMI-8226 | Growth Inhibition Assay | 10 μM | 72 h | IC50=263 nM | 23844038 |
| HuT78 | Growth Inhibition Assay | 10 μM | 72 h | IC50=52 nM | 23844038 |
| BFTC-905 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SK-N-AS | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| CHP-212 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| LS1034 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| HCC-2998 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| Calu-6 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H460 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| T-84 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H747 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| HCT-116 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| DLD-1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SW480 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SHP-77 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| A549 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| LS-174T | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| UMUC-3 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SW-837 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SW756 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| MDA-MB-231 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H508 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| OV-90 | Growth Inhibition Assay | 10 μM | 72 h | IC50=29 nM | 23844038 |
| YUMAC | Growth Inhibition Assay | 10 μM | 72 h | IC50=5 nM | 23844038 |
| WM-115 | Growth Inhibition Assay | 10 μM | 72 h | IC50=5 nM | 23844038 |
| GCT | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| A673 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| RKO | Growth Inhibition Assay | 10 μM | 72 h | IC50=2.522 μM | 23844038 |
| SW872 | Growth Inhibition Assay | 10 μM | 72 h | IC50=377 nM | 23844038 |
| SW1417 | Growth Inhibition Assay | 10 μM | 72 h | IC50=158 nM | 23844038 |
| HT-29 | Growth Inhibition Assay | 10 μM | 72 h | IC50=66 nM | 23844038 |
| ES-2 | Growth Inhibition Assay | 10 μM | 72 h | IC50=53 nM | 23844038 |
| A101D | Growth Inhibition Assay | 10 μM | 72 h | IC50=9 nM | 23844038 |
| SH-4 | Growth Inhibition Assay | 10 μM | 72 h | IC50=8 nM | 23844038 |
| SK-MEL-3 | Growth Inhibition Assay | 10 μM | 72 h | IC50=7 nM | 23844038 |
| Colo 205 | Growth Inhibition Assay | 10 μM | 72 h | IC50=7 nM | 23844038 |
| UACC-257 | Growth Inhibition Assay | 10 μM | 72 h | IC50=6 nM | 23844038 |
| DU-4475 | Growth Inhibition Assay | 10 μM | 72 h | IC50=5 nM | 23844038 |
| A375 | Growth Inhibition Assay | 10 μM | 72 h | IC50=4 nM | 23844038 |
| SK-MEL-28 | Growth Inhibition Assay | 10 μM | 72 h | IC50=3 nM | 23844038 |
| M14 | Growth Inhibition Assay | 10 μM | 72 h | IC50=2 nM | 23844038 |
| SK-MEL-1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=2 nM | 23844038 |
| C32TG | Growth Inhibition Assay | 10 μM | 72 h | IC50=1 nM | 23844038 |
| UACC-62 | Growth Inhibition Assay | 10 μM | 72 h | IC50=1 nM | 23844038 |
| MALME-3M | Growth Inhibition Assay | 10 μM | 72 h | IC50=1 nM | 23844038 |
| A375P-F11 | Growth Inhibition Assay | 10 μM | 72 h | Inhibition of B-Raf V600E mutant-driven A375P-F11 cell proliferation with IC50 of 0.071 μM | 23844038 |
| SK-MEL-28 | Growth Inhibition Assay | 10 μM | 72 h | Inhibition of B-Raf V600E mutant-driven SK-MEL-28 cell proliferation with IC50 of 0.043 μM | 23844038 |
| HFF | Growth Inhibition Assay | 10 μM | 72 h | Inhibition of proliferation of human HFF cells harboring wild type B-Raf with IC50 of 3 μM | 24900673 |
| J82 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| JM1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| Kato III | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| KHOS-240S | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| KM-12 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| KPL-1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| KYSE-30 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| LNCaP | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| MCF-7 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| MC-IXC | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| MDA-MB-175 VII | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| MDA-MB-468 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| MiaPaCa | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| Molt-4 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-ADR/RES | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H69 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H82 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-N87 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H146 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H157 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H187 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H209 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H226 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H292 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H322 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H358 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H520 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H526 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H630 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H661 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H716 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H1563 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H1792 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H2030 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H2052 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H2122 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| NCI-H2228 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| OE-19 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| OE-21 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| OE-33 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| OVCAR-3 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| OVCAR-4 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| OVCAR-5 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| P3HR-1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| PC-3 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| Raji | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| RD | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| RD-ES | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| RL | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SaOS2 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SCC-9 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SCC-12 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SCC-13 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SCC-15 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SCC-25 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SCLC-3 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SF-268 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SF-295 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SJRH30 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SK-BR-3 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SK-LMS-1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SK-N-DZ | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SK-N-F1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SKOV-3 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SK-UT-1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SN12C | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SNB-19 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SNU-5 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SNU-16 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SNU-398 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SNU-449 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SR | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| ST486 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SW579 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SW684 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SW-780 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SW900 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SW1088 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SW1463 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| SW1990 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| T47D | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| TE381.T | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| TK-10 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| U2OS | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| U251 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| UACC-812 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| YAPC | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| ZR-75-1 | Growth Inhibition Assay | 10 μM | 72 h | IC50=10 μM | 23844038 |
| A375 | Function assay | 1.2 μM | 4 h | Inhibition of phosphorylation of MEK, ERK, and S6P | 22389471 |
| Colo-205 | Function assay | 1 μM | 4 d | Induced a highly comparable compaction phenotype | 25381152 |
| M257 | Growth Inhibition Assay | 100 nM | 72 h | Does not inhibit proliferation of M257 cell harbouring wild type BRAF | 23317446 |
| LCP | Growth Inhibition Assay | 100 nM | 72 h | Inhibition of proliferation of LCP cell harbouring BRAF V600R mutantation | 23317446 |
| WM266 | Growth Inhibition Assay | 100 nM | 72 h | Inhibition of proliferation of WM266 cell harbouring BRAF V601D mutantation | 23317446 |
| M257 | Growth Inhibition Assay | 100 nM | 72 h | Does not inhibit ERK1-2 phosphorylation in M257 cell harbouring wild type BRAF | 23317446 |
| LCP | Growth Inhibition Assay | 100 nM | 72 h | Inhibit ERK1-2 phosphorylation in LCP cell harbouring BRAF V600R mutantation | 23317446 |
| WM266 | Growth Inhibition Assay | 100 nM | 72 h | Inhibit ERK1-2 phosphorylation in WM266 cell harbouring BRAF V600D mutantation | 23317446 |
| RBW-1 | Function assay | 1 μM | No reduction of Mek 1/2 phosphorylation | 24885690 | |
| RBO-1 | Function assay | 1 μM | Inhibition of Mek 1/2 phosphorylation | 24885690 | |
| RBO-2 | Function assay | 1 μM | Inhibition of Mek 1/2 phosphorylation | 24885690 | |
| RBOW | Function assay | 1 μM | Inhibition of Mek 1/2 phosphorylation | 24885690 | |
| HepG2 | Function Assay | 45 min | Inhibition of Alk5 in TGF-beta-stimulated human HepG2 cells assessed as decrease in Smad2 phosphorylation treated for 45 mins prior to TGF-beta stimulation measured after 60 mins by odyssey blot scanner analysis with IC50 of 3.7 μM | 24900673 | |
| SK-MEL-28 | Kinase Assay | 1 h | Inhibition of B-Raf V600E mutant in human SK-MEL-28 cells assessed as decrease in ERK phosphorylation with IC50 of 0.004 μM | 24900673 | |
| A375 | BRAF competitive binding assay | 15 min | IC50 = 0.006 μM | 25965804 | |
| A375 | Function assay | 72 h | IC50 = 0.011 μM | 25965804 | |
| A375 | ARAF competitive binding assay | 15 min | IC50 = 0.026 μM | 25965804 | |
| A375 | CRAF competitive binding assay | 15 min | IC50 = 0.15 μM | 25965804 | |
| A375 | Function assay | 1 h | IC50 = 0.001 μM | 27085672 | |
| MIAPaCa2 | Function assay | 1 h | EC50 = 0.529 μM | 27085672 | |
| SK-MEL-28 | Cytotoxicity assay | 72 h | IC50 = 0.043 μM | 29461827 | |
| Sf9 | Function assay | 60 min | IC50 = 0.009 μM | 27774137 | |
| SK-MEL-28 | Growth inhibition assay | 48 h | Growth inhibition of human SK-MEL-28 cells harboring BRAF V600E mutant measured after 48 hrs resazurin assay | 27774137 | |
| SK-MEL-28 | Growth inhibition assay | 48 h | Growth inhibition of human SK-MEL-28 cells harboring BRAF V600E mutant preincubated for 1 hr followed by irradiation of 1.13 kW/m2 UV-light for 5 mins measured after 48 hrs resazurin assay | 27774137 | |
| SK-MEL-28 | Cytotoxicity assay | 48 h | Cytostatic activity in human SK-MEL-28 cells harboring BRAF V600E mutant at 1 and 30 uM measured after 48 hrs resazurin assay | 27774137 | |
| COLO205 | Growth Inhibition Assay | Inhibition of human COLO205 cell proliferation with IC50 of 0.007 μM | 24900673 | ||
| HepG2 | Kinase Assay | Inhibition of B-Raf V600E mutant in human HepG2 cells assessed as decrease in ERK phosphorylation with IC50 of 0.004 μM | 24900673 | ||
| Kinase Assay | Inhibition of N-terminal His tagged B-Raf V600E mutant expressed in baculovirus infected insect cells co-expressing CDC37 assessed as decrease in biotinylated-MEK protein phosphorylation by AlphaScreen assay with IC50 of 0.0007 μM | 24900673 | |||
| YUSIT1 | Function assay | reduced sensitivity with IC50 > 0.5 μM | 22389471 | ||
| MeWo | Growth inhibition assay | IC50 = 987 nM | 26018524 | ||
| WiDr | Growth inhibition assay | IC50 = 76 nM | 26018524 | ||
| HCT116 | Function assay | IC50 = 5.88 μM | 25965804 | ||
| A375 | Function assay | IC50 = 0.004 μM | 29461827 | ||
| DAOY | Primary screen assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| NB1643 | Primary screen assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| SK-N-MC | Primary screen assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Dabrafenib是一种突变型BRAFV600E特异性抑制剂，无细胞试验中IC50为0.7 nM，作用于B-Raf(wt)和c-Raf效果分别低7和9倍。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Dabrafenib对Raf激酶具有选择性，对B-Raf的活性比其它测试过的91%的激酶高400倍。 Dabrafenib抑制B-RafV600E激酶，导致ERK磷酸化降低和抑制细胞的增值，在特异性编码突变的B-RafV600E的癌细胞中细胞停滞在G1期。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | pMEK / pERK / ERK p-S6 / p-AKT308 / p-AKT473 β-catenin |
|
31158244 | |
| Growth inhibition assay | IC50 |
|
24735930 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Dabrafenib（口服）抑制B-RafV600E突变的黑色素瘤（A375P）的生长，在免疫受损小鼠中皮下注射结肠癌（Colo205），Dabrafenib（口服）同样能抑制肿瘤生长。 [1] |
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|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06079333 | Recruiting | Anaplastic Thyroid Cancer |
Leiden University Medical Center|Novartis |
January 1 2023 | Phase 2 |
| NCT06337617 | Completed | BRAF V600 Mutation Positive Melanoma |
Novartis Pharmaceuticals|Novartis |
May 10 2022 | -- |
| NCT04961619 | Recruiting | Melanoma |
Novartis Pharmaceuticals|Novartis |
December 1 2021 | -- |
| NCT04547946 | Completed | Malignant Melanoma |
Novartis Pharmaceuticals|Novartis |
October 15 2021 | -- |
| NCT05171374 | Recruiting | Melanoma Stage III|Melanoma Stage IV|Melanoma |
MelanomaPRO Russia|Novartis |
September 30 2021 | -- |
化学信息&溶解度
| 分子量 | 519.56 | 分子式 | C23H20F3N5O2S2 |
| CAS号 | 1195765-45-7 | SDF | Download Dabrafenib SDF |
| Smiles | CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (192.47 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 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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