Chemical Structure : IDH305
CAS No.: 1628805-46-8
Catalog No.: 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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IDH 305 (IDH305) is a potent, selective, brain penetrant mutant IDH1 inhibitor with IC50 of 18 and 28 nM for IDH1 R132H and R132C; exhibits >200 fold selectivity over WT IDH1 (IC50=6.14 uM), and no activtiy against IDH2 mutants; inhibits EGF-independent proliferation of HCT116-IDH1R132H+/- cells with IC50 of 20 nM; exhibits in vivo correlation of 2-HG reduction and efficacy in IDH1 mutant xenograft tumor model.
Brain Cancer
Phase 1 Clinical
M.Wt | 490.463 | |
Formula | C23H22F4N6O2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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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 |
1. Cho YS, et al. ACS Med Chem Lett. 2017 Sep 18;8(10):1116-1121.
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