1195765-45-7达拉菲尼,达帕菲尼

达拉菲尼,达帕菲尼
分子式：C23H20F3N5O2S2
分子量：519.56
产品描述
Dabrafenib(GSK2118436) 是突变型BRAFV600 特异性YZ剂，IC50为0.8 nM,作用于B-Raf(wt)和c-Raf效果低4和6倍。
靶点
B-rafB-RafV600Ec-Raf IC503.2 nM0.8 nM5.0 nM
体外研究
Dabrafenib is selective for Raf kinase, with 400 fold selectivity towards B-Raf over 91% of the other kinases tested. Dabrafenib inhibits B-RafV600E kinase, leading to decreased ERK phosphorylation and inhibition of cell proliferationby an initial arrest in the G1 phase of the cell cycle in cancer cells that specifically encode the mutation for B-RafV600E.
体内研究
Dabrafenib (orally administrated) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice.溶解性DMSO 30 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
稳定性
2年 -20°C粉状，6月-80°C溶于DMSO