GSK973

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GSK973

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:

2138473-38-6

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，pK_d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; pK_d=8.3~8.5)。

生物活性

GSK973 is a highly selective, orally bioavailable inhibitor of theBD2s(second bromodomains) of the BET family, with apIC₅₀of 7.8 and apK_dof 8.7 forBRD4BD2. GSK973 displays a 1600-fold selectivity forBRD4BD2 overBRD4BD1. GSK973 shows good potency againstBRD2BD2,BRD3BD2, andBRDTBD2 (pIC₅₀=7.4~7.8; pK_d=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, CI_renal, V_ss, and T_1/2are 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 F_poof 48%^[1].

Animal Model:	Male Wistar Han Rats^[1]
Dosage:	1 mg/kg (Pharmacokinetic Analysis)
Administration:	I.v.
Result:	The CL, CI_renal, V_ss, and T_1/2were 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.