|Solubility:||DMSO up to 100 mM; EtOH up to 100 mM|
|Storage:||Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.|
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.
- 1. Erica Hansen, et al. AG-120, an Oral, Selective, First-in-Class, Potent Inhibitor of Mutant IDH1, Reduces Intracellular 2HG and Induces Cellular Differentiation in TF-1 R132H Cells and Primary Human IDH1 Mutant AML Patient Samples Treated Ex Vivo. (2014) Blood. 124:3734
- 2. Kc B, et al. Evidence for Clinical Differentiation and Differentiation Syndrome in Patients With Acute Myeloid Leukemia and IDH1 Mutations Treated With the Targeted Mutant IDH1 Inhibitor, AG-120. (2016) Clin Lymphoma Myeloma Leuk. In press.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.