Biological Activity:AG-120 (Ivosidenib) is a potent, selective and reversible inhibitor of IDH1 with IC50 < 100 nM. It has been shown to lower 2-HG levels and restore cellular differentiation in IDH1-mutant primary human blast cells cultured ex vivo. In phase I clinical trials targeting patients with IDH1-mutated, relapsed and/or refractory (R/R) AML or untreated AML not eligible for standard of care or R/R MDS, AG-120 is well tolerated to date (10/2015) and MTD was not reached. Overall response rate is 35% including 12 CRs.How to Use:In vitro: AG-120 was used at 1 µM in vitro and cellular assays. In vivo: AG-120 was dosed orally to mice bearing IDH1 mutant tumors at 150 mg/Kg once per day. Reference:
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