IDH1 Inhibitor 1 (C09-1139-908)

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 ). Specification: 0.99 Molecular Formula: C20H18F4N6O2 Molecular Weight: 450.39 PubChem CID: 137333448 Isomeric SMILES: C[C@@H](C1=CN(C=N1)C2=CC=C(C=C2)C(F)(F)F)NC3=NC=CC(=N3)N4[C@H](COC4=O)CF