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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Isocitrate Dehydrogenase (IDH)-IDH889
IDH889

Chemical Structure : IDH889

CAS No.: 1429179-07-6

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IDH889 (IDH 889;IDH-889)

货号: PC-35173Not For Human Use, Lab Use Only.

IDH889 (IDH-889) is a potent, selective, brain penetrant, orally active IDH1 R132H mutant with IC50 of 20 nM, with good overall selectivity vs the wt IDH1.

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5 mg ￥2580 In stock
10 mg ￥3980 In stock
25 mg ￥5980 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

IDH889 (IDH-889) is a potent, selective, brain penetrant, orally active IDH1 R132H mutant with IC50 of 20 nM, with good overall selectivity vs the wt IDH.
IDH889 binds into an allosteric, induced-fit pocket in IDH1R132H, shows potent cellular inhibition of 2-HG production in the engineered HCT116-IDH1R132H cell line with IC50 of 14 nM.
IDH889 inhibits 2-HG inhibition, modulates mutant IDH1-dependent DNA methylation changes in vivo.
IDH889 causes time-dependent changes, preferential hypomethylation of the loci in mutant cells.
IDH889 shows robust reduction of tumor derived 2-HG in a murine IDH1 mutant tumor xenograft model.
In addition to the potential treatment of AML, chondrosarcoma, cholangiocarcinoma, and other forms of mutant-IDH1 driven cancers, IDH889 demonstrates brain penetrant exposure.

物理化学性质&存储条件

分子量 436.491
分子式 C23H25FN6O2
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

(S)-3-(2-(((S)-1-(5-(4-fluoro-3-methylphenyl)pyrimidin-2-yl)ethyl)amino)pyrimidin-4-yl)-4-isopropyloxazolidin-2-one

参考文献

1. Levell JR, et al. ACS Med Chem Lett. 2016 Dec 16;8(2):151-156.

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