Olutasidenib 是一种可透过血脑屏障的、具有口服活性的、突变型异柠檬酸脱氢酶(IDH)1的选择性有效抑制剂，对IDH1- R132H 和 IDH1- R132C的IC50分别为 21.2 nM 和 114 nM，可用于急性髓性白血病或骨髓增生异常综合征的研究。

Olutasidenib is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS). Olutasidenib is a highly effective, brain penetrant, and selective inhibitor of the mutant Isocitrate dehydrogenase 1 (IDH1) (IC50: 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively).

Olutasidenib is highly selective for IDH1 isoforms, showing no appreciable inhibition against wild-type IDH1 (>20 μM) and IDH2 mutants (R172K and R140Q: both >20 μM). Olutasidenib effectively suppresses 2-HG production by multiple IDH1-R132 mutants (R132H, R132C, R132G, R132L), displaying Olutasidenib (FT-2102) could be efficacious against most IDH1-R132 mutant-expressing tumors [2].

In HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice, Olutasidenib (three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals) shows effective anti-tumor activity [2].

1887014-12-1

C18H15ClN4O2

354.79

FT-2102

DMSO:122 mg/mL (343.87mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years