中文名：奥塔西德尼（FT-2102）
英文名：Olutasidenib (FT-2102)
纯度：Moligand™，≥98%
货号：O414289
Cas号：1887014-12-1
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
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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关键字： D87221 ; 0T4IMT8S5Z ; FT-2102FT-2102 ; AC-36556
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