AGI-14100

AGI-14100 (AGI14100) is a novel potent and selective, orally available IDH1 mutant inhibitor; inhibits cell proliferation (human cell lines transfected with IDH1 R132H) with IC50 values of 0.76 nM (HT-1080), 0.74 nM (U87-MG) and 1.75 nM (TF1); AGI-14100 can specifically induce cellular differentiation in AML patient samples with mutant IDH1 ex vivo; significantly reduces the leukemic blast burden in the peripheral blood in xenograft model with a primary human IDH1 R132H/FLT3-ITD tumor.

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)