2234285-81-3
中文名稱
IDH1 INHIBITOR 1
英文名稱
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 結(jié)構(gòu)式
基本信息
中文別名
化合物 T11613 英文別名
IDH1 Inhibitor 12-Oxazolidinone, 4-(fluoromethyl)-3-[2-[[(1S)-1-[1-[4-(trifluoromethyl)phenyl]-1H-imidazol-4-yl]ethyl]amino]-4-pyrimidinyl]-, (4R)-
常見問題列表
生物活性
IDH1 Inhibitor 1 是一種有效的，口服生物可利用的，腦滲透性，選擇性突變 IDH1 抑制劑，抑制 IDH1R132H，IDH1R132C，和 IDH1WT，IC50 分別為 0.021 μM, 0.045 μM, 和 2.52 μM。具有抗腫瘤活性。靶點(diǎn)
IC50: 0.021 μM (IDH1 R132H ), 0.045 μM (IDH1 R132C ), and 2.52 μM (IDH1 WT )
體外研究
IDH1 Inhibitor 1 (Compound 19) inhibits cellular HCT116-IDH1 R132H/+ with an IC 50 of 0.039 μM.
體內(nèi)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.