| 产品编号 |
产品名称 |
产品包装 |
产品价格 |
| SD7252-10mM |
Enasidenib (Dehydrogenase抑制剂) |
10mM |
149.00元 |
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
|
参考文献：
1. Alan H. Shih, et al. Blood. 2014, 124:437.
2. Kate Ellwood-Yen, et al. AACR. 2014, 74(19 Sup.):3116.
包装清单：
|
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。
注意事项：
本产品对人体有害，操作时请小心，并注意有效防护以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。