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CAS No.: 1300031-52-0

GSK1324726A Catalog No. CSN16910

Synonyms: I-BET726

GSK1324726A is an inhibitor of BET proteins BRD2, BRD3, BRD4 with IC50 of 41 nM, 31 nM, and 22 nM respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Bromodomain 4

IC50:22nM Bromodomain 3

IC50:31nM Bromodomain 2

IC50:41nM
描述GSK1324726A works as both a selective BET Bromodomain inhibitor with pIC50 values of 7.4, 7.1, 7 and 7.3 for BRD2, BRD3, BRD4 and BRDT, respectively, and a potent tetrahydroquinoline ApoA1 up-regulator. It inhibited the production of LPS-stimulated IL6 with pIC50 values of 7.3 and 6.4 in PBMC and HWB cells, respectively. Oral administration of GSK1324726A at doses of 3mg/kg and 10mg/kg significantly reduced expression of PAI-1 mRNA in a murine acute LPS challenge model. Intravenous injection with GSK1324726A at dose of 10mg/kg increased the ratio of survival of a murine septic shock model^[3].
作用机制GSK1324726A binds to the acetyl-lysine pocket.^[3]

动物研究

剂量

Mice: 5 mg/kg, 15 mg/kg^[2] (p.o.); 10 mg/kg^[1] (i.v.) Rat: 1 mg/kg^[1] (i.v.); 3 mg/kg^[1] (p.o.)

给药途径

p.o., i.v.

动物药代数据

Animal	Mice^[1]	Rats^[1]	Dogs^[1]	Monkeys^[1]
Dose	10 mg/kg (i.v.) 3 mg/kg (p.o.)	1 mg/kg (i.v.) 3 mg/kg (p.o.)	1 mg/kg (i.v.) 3 mg/kg (p.o.)	1 mg/kg (i.v.) 2 mg/kg (p.o.)
Administration	i.v. p.o.	i.v. p.o.	i.v. p.o.	i.v. p.o.
F	45% (p.o.)	28 ± 1% (p.o.)	80 ± 12% (p.o.)	103 ± 35% (p.o.)
CL_b	3.1 ± 0.4 ml/min/kg (i.v.)	26 ± 4 ml/min/kg (i.v.)	6.0 ± 1 ml/min/kg (i.v.)	3.0 ± 0.9 ml/min/kg (i.v.)
T_1/2	3.6 ± 0.2 h (i.v.)	> 8 h (i.v.)	1.8 ± 0.6 h (i.v.)	2.7 ± 0.1 h (i.v.)
Vss	0.48 ± 0.1 L/kg (i.v.)	2.0 ± 0.4 L/kg (i.v.)	0.8 ± 0.1 L/kg (i.v.)	1.0 ± 0.4 L/kg (i.v.)
AUC_0→t	6028 ng·h/ml (p.o.)	539 ± 96 ng·h/ml (p.o.)	5900 ± 968 ng·h/ml (p.o.)	10968 ± 3852 ng·h/ml (p.o.)

参考文献

[1] Gosmini R, Nguyen VL, et al. The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem. 2014 Oct 9;57(19):8111-31.
[2] Wyce A, Ganji G, et al. BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models. PLoS One. 2013 Aug 23;8(8):e72967.
[3] Gosmini R, Nguyen VL, Toum J, Simon C, Brusq JM, Krysa G, Mirguet O, Riou-Eymard AM, Boursier EV, Trottet L, Bamborough P, Clark H, Chung CW, Cutler L, Demont EH, Kaur R, Lewis AJ, Schilling MB, Soden PE, Taylor S, Walker AL, Walker MD, Prinjha RK, Nicodème E. The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor. J Med Chem. 2014 Oct 9;57(19):8111-31. doi: 10.1021/jm5010539. Epub 2014 Sep 24. PMID: 25249180.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2993 mL
- 11.4965 mL
- 22.9930 mL
- 5 mM
- 0.4599 mL
- 2.2993 mL
- 4.5986 mL
- 10 mM
- 0.2299 mL
- 1.1497 mL
- 2.2993 mL

技术信息

CAS号

1300031-52-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H23ClN2O3

运输

蓝冰

分子量

434.91

别名

I-BET726

溶解度

DMSO	85.0 mg/mL (195.4 mM)
Water	Insoluble
Ethanol	85.0 mg/mL (195.4 mM)

动物实验配方

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靶点	Description	IC50
Bromodomain 4		IC50:22nM
Bromodomain 3		IC50:31nM
Bromodomain 2		IC50:41nM

GSK1324726A Catalog No. CSN16910

靶点选择性

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