AGI-14100

AGI-14100(AGI14100)是一种新型有效且选择性的口服IDH1突变体抑制剂；抑制细胞增殖(用IDH1 R132H转染的人细胞系),IC50值为0.76 nM(HT-1080),0.74 nM(U87-MG)和1.75 nM(TF1)；AGI-14100可以离体诱导具有突变体IDH1的AML患者样品中的细胞分化；显着降低具有原代人IDH1 R132H/FLT3-ITD肿瘤的异种移植模型中外周血中的白血病爆炸负荷。

References 1. Ma T, et al. J Med Chem. 2018 Jun 18. doi: 10.1021/acs.jmedchem.8b00159. 2. Kate Ellwood-Yen, et al. Abstract 1194: IDH1 mutant inhibitor induces cellular differentiation and offers a combination benefit with Ara-C in a primary human Idh1 mutant AML xenograft model. AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA. View Related Products by Target Isocitrate Dehydrogenase (IDH)