产品详情
简单介绍：
AG-120(Ivosidenib),IDH1Inhibitor
详情介绍：
Product Information
| Molecular Weight: | 582.96 |
| Formula: | C28H22ClF3N6O3 |
| Purity: | ≥98% |
| CAS#: | 1448347-49-6 |
| Solubility: | DMSO up to 100 mM; EtOH up to 100 mM |
| Chemical Name: | (S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
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:
- 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.
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