化学信息：
| 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 |
|
| 简称 | Enasidenib | |
| 别名 |
AG-221, CC-90007, GTPL8960, CS-5017, AK431837 |
|
| 中文名 | N/A | |
| 化学式 | C19H17F6N7O | |
| 分子量 | 473.38 | |
| CAS号 | 1446502-11-9 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO100mg/ml; Ethanol100mg/ml |
|
| 溶液配制 | 5mg加入1.06ml DMSO，或者每4.73mg加入1ml DMSO，配制成10mM溶液。SD7252-10mM用DMSO配制。 |
生物信息：
| 产品描述 | Enasidenib is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme. | ||||
| 信号通路 | Metabolism | ||||
| 靶点 | IDH2 | － | － | － | － |
| IC50 | 12nM | － | － | － | － |
| 体外研究 | The compound has been demonstrated to reduce 2-HG levels by >90% and reverse histone and deoxyribonucleic acid (DNA) hypermethylation in vitro, and to induce differentiation in leukemia cell models. | ||||
| 体内研究 | AG-221 is able to potently reduce 2HG found in the bone marrow, plasma and urine of engrafted mice. Treatment also induced a dose dependent, statistically significant, survival benefit. A proliferative burst of the human specific CD45+ blast cells is followed by cellular differentiation as measured by the expression of CD11b, CD14 and CD15 and cell morphology after AG-221 treatment. AG-221 treatment also restores megakaryocyte-erythroid progenitor (MEP) differentiation that is suppressed by mutant IDH2 expression and reverses the effects of mutant IDH2 on DNA methylation in mutant stem/progenitor cells. Clinical trials combining IDH2 inhibitors with other targeted Aml therapies are warranted in order to increase therapeutic efficacy. | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | N/A |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | Murine models of IDH2-mutant leukemia |
| 配制 | N/A |
| 剂量 | 10mg/kg or 100mg/kg bid |
| 给药方式 | N/A |
| 产品编号 | 产品名称 | 包装 |
| SD7252-10mM | Enasidenib (Dehydrogenase抑制剂) | 10mM×0.2ml |
| SD7252-5mg | Enasidenib (Dehydrogenase抑制剂) | 5mg |
| SD7252-25mg | Enasidenib (Dehydrogenase抑制剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
