2234285-81-3

中文名称 IDH1 INHIBITOR 1

英文名称 IDH1 Inhibitor 1

CAS 2234285-81-3

分子式 C20H18F4N6O2

分子量 450.39

MOL 文件 2234285-81-3.mol

2234285-81-3 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T11613

英文别名

IDH1 Inhibitor 1
2-Oxazolidinone, 4-(fluoromethyl)-3-[2-[[(1S)-1-[1-[4-(trifluoromethyl)phenyl]-1H-imidazol-4-yl]ethyl]amino]-4-pyrimidinyl]-, (4R)-

物理化学性质

储存条件4°C, away from moisture and light

形态Solid

颜色White to off-white

常见问题列表

生物活性

IDH1 Inhibitor 1 是一种有效的，口服生物可利用的，脑渗透性，选择性突变 IDH1 抑制剂，抑制 IDH1R132H，IDH1R132C，和 IDH1WT，IC50 分别为 0.021 μM, 0.045 μM, 和 2.52 μM。具有抗肿瘤活性。

靶点

IC50: 0.021 μM (IDH1 ^R132H ), 0.045 μM (IDH1 ^R132C ), and 2.52 μM (IDH1 ^WT )

体外研究

IDH1 Inhibitor 1 (Compound 19) inhibits cellular HCT116-IDH1 ^R132H/+ with an IC ₅₀ of 0.039 μM.

体内研究

IDH1 Inhibitor 1 (Compound 19) inhibits 2-hydroxyglutarate (2-HG) production in a preclinical xenograft tumor model. IDH1 Inhibitor 1 is also profiled in a patient-derived IDH1 mutant HCT116-IDH1 ^R132H/+ mechanistic xenograft tumor model in mice to evaluate in vivo inhibition of 2-HG production. IDH1 Inhibitor 1, dosed orally at 150 mg/kg, inhibits new 2-HG production.