IDH-305 是突变选择性的、口服性的、脑渗透性的IDH1抑制剂，靶向 IDH1 (R132) 突变。它对突变体 IDH1 亚型的选择性比野生型高 200 倍 (IC50= 27 nM (IDH1R132H), 28 nM (IDH1R132C), 6.14 μM (IDH1WT))。

IDH-305 is an orally available, mutation-selective, and brain-penetrant IDH1 inhibitor targeting the IDH1 (R132) mutation. IDH-305 is 200-fold more selective for mutant IDH1 isoforms than wild type with IC50s of 27 nM,28 nM and 6.14 nM for IDH1R132H, IDH1R132C and IDH1WT, respectively.

IDH-305 suppresses HCT116-IDH1R132H /- cells (IC50 of 24 nM)[1].

P.o. administration of 30-300 mg/kg IDH-305 twice daily for 21 days suppresses 2-HG production and 2-HG-dependent tumor growth of an IDH1 mutant PDX melanoma model [1].

1628805-46-8

C23H22F4N6O2

490.45

DMSO:100 mg/mL (203.90 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years