GSK973

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GSK973 

GSK973 是 BET 家族 BD2s 的高选择性口服生物利用度抑制剂，对 BRD4 BD2 的pIC50 为 7.8，pKd 为8.7。GSK973 显示 BRD4 BD2 的选择性是 BRD4 BD1 的1600 倍。GSK973 对 BRD2-BD2、BRD3-BD2 和 BRDT-BD2 有很好的抑制作用 (pIC50=7.4~7.8; pKd=8.3~8.5)。

GSK973

GSK973 Chemical Structure

CAS No. : 2138473-38-6

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生物活性

GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5)[1].

IC50 & Target[1]

BRD4 BD2

7.8 (pIC50)

BRD2 BD2

7.5 (pIC50)

BRD3 BD2

7.8 (pIC50)

BRDT BD2

7.4 (pIC50)

BRD4 BD2

8.7 (pKd)

BRD2 BD2

8.3 (pKd)

BRD3 BD2

8.5 (pKd)

BRDT BD2

8.3 (pKd)

体内研究
(In Vivo)

GSK973 (1 mg/kg; i.v.) treatment shows the CL, CIrenal, Vss, and T1/2 are 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively[1].
GSK973 (3 mg/kg; p.o) treatment shows the Fpo of 48%[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar Han Rats[1]
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: I.v.
Result: The CL, CIrenal, Vss, and T1/2 were 73 mL/min/kg, 4 mL/min/kg, 2.1L/kg, and 0.6 hours, respectively.

分子量

410.44

Formula

C23H23FN2O4
CAS 号

2138473-38-6
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.
参考文献

  • [1]. Preston A, et al. GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family. ACS Med Chem Lett. 2020;11(8):1581-1587. Published 2020 Jul 6.

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