Information Olutasidenib (FT-2102) Olutasidenib is a potent, orally bioavailable, brain penetrant and selective mutant IDH1 (mIDH1) inhibitor with IC50 of 21.1 nM, 114 nM for IDH1-R132H , IDH1-R132C , respectively. Targets IDH1 (R132H) (Cell-free assay); IDH1 (R132C) (Cell-free assay) 21.1 nM; 114 nM In vitro Profiling in various mIDH1 over-expressing U87 cells and HCT116 cells reveals that olutasidenib potently inhibits 2-HG production by multiple IDH1-R132 mutants (R132H, R132C, R132G, R132L), suggesting olutasidenib could be efficacious against most IDH1-R132 mutant-expressing tumors. Olutasidenib is highly selective for IDH1 isoforms, showing no appreciable inhibition against wild-type IDH1 and IDH2 mutants.. In vivo In IDH1-R132H/ xenograft models, the free concentration of Olutasidenib is comparable in plasma and xenograft tumors, and exposures are dose-dependent. In comparison to the vehicle treated group, Olutasidenib shows a time and dose-dependent inhibition of 2-HG levels in tumor. Calculations based upon the percentage of suppression of 2-HG concentration in tumor versus the free drug concentration in tumor give in vivo IC50 values of 26 nM and 36 nM in the HCT116-IDH1-R132H or HCT116-IDH1-R132C models, respectively. Olutasidenib has good cell permeability and low efflux ratio in the male CD-1 mouse, which indicate a low probability of p-glycoprotein driven efflux.. Cell Research(from reference) Cell lines：HCT116-IDH1-R132H/+, HCT116-IDH1-R132C/+, HT1080, U87MG cells Incubation Time：24 h
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Olutasidenib (FT-2102)
CAS number：1887014-12-1 molecular formula：C18H15ClN4O2
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| Chinese alias | - | ||
| English alias | Olutasidenib | 1887014-12-1 | FT-2102 | Rezlidhia | 0T4IMT8S5Z | Olutasidenib [USAN] | 5-[[(1S)-1-(6-chloro-2-oxo-1H-quinolin-3-yl)ethyl]amino]-1-methyl-6-oxopyridine-2-carbonitrile | FT2102 | (S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino | ||
| CAS number | 1887014-12-1 | molecular formula | C18H15ClN4O2 |
| molecular weight | 354.79 g/mol | Exact mass | - |
| PSA | 85.200 Ų | logp | 1.234 |
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