產(chǎn)品屬性：

Cas No.1446502-11-9

別名 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

化學(xué)名

分子式 C19H17F6N7O

分子量 473.37

溶解度 ≥ 47.3mg/mL in DMSO

儲存條件 Store at -20°C
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
產(chǎn)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].