Olutasidenib

Research use only, not for human use.

Olutasidenib (FT-2102, FT2102) is an oral, highly potent, selective small molecule inhibitor of mutated IDH1 R132.

Olutasidenib (FT-2102, FT2102) is an oral, highly potent, selective small molecule inhibitor of mutated IDH1 R132; specifically inhibits IDH1(R132), thereby inhibiting the formation of the oncometabolite 2-hydroxyglutarate (2HG) from alpha-ketoglutarate (a-KG). This prevents 2HG-mediated signaling and leads to both an induction of cellular differentiation and an inhibition of cellular proliferation in tumor cells expressing IDH(R132).Blood Cancer Phase 2 Clinical(In Vivo):Olutasidenib (FT-2102, three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals) exhibits potent anti-tumor activity in HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice.

Olutasidenib (FT-2102) potently inhibits 2-HG production by multiple IDH1-R132 mutants (R132H, R132C, R132G, R132L), suggesting Olutasidenib (FT-2102) could be efficacious against most IDH1-R132 mutant-expressing tumors. Olutasidenib (FT-2102) 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 (FT-2102, three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals) exhibits potent anti-tumor activity in HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice. Animal Model:HCT116-IDH1-R132H/+ xenograft bearing female BALB/c Nude mice.Dosage:12.5, 25, and 50 mg/kg.Administration:Three oral doses (12.5, 25, and 50 mg/kg) in 12-hour intervals.Result:Showed a time and dose-dependent inhibition of 2-HG levels in in tumor.At the highest dose tested in these studies (50 mg/kg), treatment with FT-2102 inhibited 2-HG levels in the tumor by >90% for up to 24 hours after the last dose in the HCT116-IDH1-R132H/+ xenograft model.

FT-2102 | FT2102

Metabolic Enzyme/Protease

IDH

IDH

Cancer

Blood cancer

1887014-12-1

354.794

C18H15ClN4O2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (352.32 mM)

N#CC1=CC=C(N[C@H](C2=CC3=C(NC2=O)C=CC(Cl)=C3)C)C(N1C)=O

5-[[(1S)-1-(6-Chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl]amino]-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years