GSK040 是一种有效和具有选择性的BET BD2抑制剂，pIC50值为 8.3。GSK040 对 BET BD2 的选择性比 BET BD1 (pIC50=4.6) 高 5000 倍。GSK040 可用于肿瘤学和免疫学疾病的研究。
产品描述
GSK040 is a potent and highly selective BET BD2 inhibitor, with a pIC 50 of 8.3. GSK040 shows more than 5000-fold selectivity for BET BD2 over BET BD1 (pIC 50 =4.6). GSK040 can be used for the research of oncology and immunology diseases [1].
体内活性
GSK040 (1 mg/kg; i.v.) exhibits t 1/2 (0.19 h), CLb (50 mL/min/kg) and Vss (0.6 L/kg) in rats [1]. GSK040 (3 mg/kg; p.o.) exhibits oral bioavailability (16%), t max (0.25 h), C max (398 nM) in rats [1].
分子式
C29H34N4O4
分子量
502.6
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
