GSK040

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GSK040

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2752331-09-0

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。

生物活性

GSK040 is a potent and highly selectiveBETBD2inhibitor, with apIC₅₀of 8.3. GSK040 shows more than 5000-fold selectivity for BETBD2over BETBD1(pIC₅₀=4.6). GSK040 can be used for the research of oncology and immunology diseases^[1].

IC₅₀& Target^[1]

BD2

8.3 (pIC₅₀)

体内研究
(In Vivo)

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].

分子量

502.60

Formula

C₂₉H₃₄N₄O₄

CAS 号

2752331-09-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.