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Chemical Structure : IDH889
CAS No.: 1429179-07-6
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $258 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $598 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 436.491 | |
| Formula | C23H25FN6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Levell JR, et al. ACS Med Chem Lett. 2016 Dec 16;8(2):151-156.
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