DS-1001b
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1898207-64-1
≥98%
A crystalline solid
608.9
(2e)-3-[1-[[5-(1-fluoro-1-methylethyl)-3-(2,4,6-trichlorophenyl)-4-isoxazolyl]carbonyl]-3-methyl-1h-indol-4-yl]-2-propenoic acid, compd. with 2-methyl-2-propanamine (1:1)
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- MSDS: View or download
An inhibitor of mutant IDH1 (IC50s = 15 and 130 nM for IDH1R132H and IDH1R132C, respectively); selective for mutant IDH1 over wild-type IDH1 and IDH2, as well as IDH2R140Q and IDH2R172Q (IC50s = >10,000 nM for all); inhibits 2-HG production in TF-1 cells stably transfected with IDH1R132H or IDH1R132C (IC50s = 29 and 35 nM, respectively) and in 293A cells transiently transfected with IDH1R132H or IDH1R132C (IC50s = 29 and 42 nM, respectively); reduces tumor growth, as well as intratumoral and plasma 2-HG levels, in a subcutaneous IDH1R132H-expressing A1074 PDX mouse model of glioblastoma
-20°C