• 生物活性

靶点及简介 ：mutant IDH1 inhibitor

Ivosidenib (AG-120) 是一种具有口服活性的异柠檬酸脱氢酶（IDH1）抑制剂，具有潜在的抗肿瘤活性。Ivosidenib特异性地抑制细胞质中突变形式的IDH1，从而抑制了代谢物2-羟基戊二酸（2HG）的形成。

在体外研究中，用Ivosidenib (AG-120)处理TF-1细胞和携带突变IDH1的初级人类AML患者样品，降低了细胞内2-HG水平、抑制了不依赖于生长因子的细胞增殖以及恢复TF-1 IDH1-R132H细胞中由红细胞生成素所诱导的细胞分化。

• 验证及参考文献

验证：

参考文献：

[1]. Agresta Samuel V, et al. (S)-N-((S)-1-(2-Chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide as therapeutically active compound for treating cancer characterized by a mutant allele of IDH1. From PCT Int. Appl. (2015), WO 2015127172 A1 20150827.

[2]. Gu Chong-Hui, et al. Pharmaceutical compositions of therapeutically active compounds comprising (S)-N-((S)-1-(2-chlorophenyl)-2-[(3,3-difluorocyclobutyl)amino]-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide for treating hematologic malignancies with mutant allele of IDH1. From PCT Int. Appl. (2015), WO 2015138839 A1 20150917

• 溶解度及制备方案

DMSO	100 mg/mL (171.54 mM)
Ethanol	100 mg/mL (171.54 mM)
Water	Insoluble

制备储备液

浓度 溶剂体积  质量	1 mg	5 mg	10 mg
1 mM	1.7154 mL	8.5769 mL	17.1538 mL
5 mM	0.3431 mL	1.7154 mL	3.4308 mL
10 mM	0.1715 mL	0.8577 mL	1.7154 mL
50 mM	0.0343 mL	0.1715 mL	0.3431 mL

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