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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Isocitrate Dehydrogenase (IDH)-IDH305
IDH305

Chemical Structure : IDH305

CAS No.: 1628805-46-8

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IDH305 (IDH-305;IDH 305)

货号: PC-60164Not For Human Use, Lab Use Only.

IDH 305 (IDH305) is a potent, selective, brain penetrant mutant IDH1 inhibitor with IC50 of 18 and 28 nM for IDH1 R132H and R132C.

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5 mg ￥1380 In stock
10 mg ￥2280 In stock
25 mg ￥3780 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

IDH305 (IDH-305) is a potent, selective, brain penetrant mutant IDH1 inhibitor with IC50 of 18 and 28 nM for IDH1 R132H and R132C.
IDH305 exhibits >200 fold selectivity over WT IDH1 (IC50=6.14 uM), and no activtiy against IDH2 mutants.
IDH305 inhibits EGF-independent proliferation of HCT116-IDH1R132H+/- cells with IC50 of 20 nM.
IDH305 exhibits in vivo correlation of 2-HG reduction and efficacy in IDH1 mutant xenograft tumor model.

物理化学性质&存储条件

分子量 490.463
分子式 C23H22F4N6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(R)-4-((S)-1-fluoroethyl)-3-(2-(((S)-1-(4-methyl-2'-(trifluoromethyl)-[3,4'-bipyridin]-6-yl)ethyl)amino)pyrimidin-4-yl)oxazolidin-2-one

参考文献

1. Cho YS, et al. ACS Med Chem Lett. 2017 Sep 18;8(10):1116-1121.

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