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Olutasidenib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Olutasidenib图片
CAS NO:1887014-12-1
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
FT-2102
产品介绍
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。

产品描述

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).

体外活性

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].

体内活性

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].

Cas No.

1887014-12-1

分子式

C18H15ClN4O2

分子量

354.79

别名

FT-2102

储存和溶解度

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