aladdin 阿拉丁 O414289 奥塔西德尼（FT-2102） 1887014-12-1 98%

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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