IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT ( IC 50 = 27 nM ( IDH1 R132H ), 28 nM ( IDH1 R132C ), 6.14 µM ( IDH1 WT )).
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