Description
IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC 50 s of 0.021 µM, 0.045 µM, and 2.52 µM for IDH1 R132H, IDH1 R132C, and IDH1 WT, respectively Anticancer activityIn VitroIDH1 Inhibitor 1 (Compound 19) inhibits cellular HCT116-IDH1 R132H/+ with an IC 50 of 0.039 µM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoIDH1 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:IC50: 0.021 µM (IDH1 R132H ), 0.045 µM (IDH1 R132C ), and 2.52 µM (IDH1 WT )