| CAS NO: | 1446502-11-9 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| 100mg | 电议 |
| Cas No. | 1446502-11-9 |
| 别名 | 恩西地平; AG-221 |
| 化学名 | 2-methyl-1-((4-(6-(trifluoromethyl)pyridin-2-yl)-6-((2-(trifluoromethyl)pyridin-4-yl)amino)-1,3,5-triazin-2-yl)amino)propan-2-ol |
| Canonical SMILES | CC(O)(C)CNC1=NC(C2=NC(C(F)(F)F)=CC=C2)=NC(NC3=CC(C(F)(F)F)=NC=C3)=N1 |
| 分子式 | C19H17F6N7O |
| 分子量 | 473.37 |
| 溶解度 | ≥ 47.3mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | IC50: ~16 nM for IDH2 R140Q mutant AG-221 (Enasidenib) is a mutant isocitrate dehydrogenase 2 (IDH2) inhibitor. The somatic mutations of IDH1 and IDH2 are found in patients with acute myeloid leukemia. Leukemia-associated IDH1/2 mutations lead to aberrant accumulation of the oncometabolite 2-hydroxyglutarate (2-HG). In vitro: AG-221 was found to be able to reduce 2-HG levels by >90%, reverse in-vitro histone and DNA hypermethylation, and induce differentiation in leukemia cell model as well. In addition, a dose dependent proliferative burst of the human specific CD45+ blast cells was observed by the treatment of AG-221, as measured by the expression of CD11b, CD14, CD15 and cell morphology [1]. In vivo: The efficacy of AG-221 in a primary human AML xenograft model with the IDH2 R140Q mutation was studied, and the results showed that AG-221 could reduce 2-HG in the plasma, bone marrow, and urine of engrafted mice potently. In addition, the treatment of AG-221 could also induce a significant and dose dependent survival benefit as demonstrated by that all mice in the high dose treatment of AG-221 survived to the end of study [1]. Clinical trial: A phase 1, multicenter, dose-escalation, safety, PK, PD, and clinical activity study of AG-221 in patients with advanced hematologic malignancies with an IDH2 mutation has been conducted [2]. References: |
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