化学信息：
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化学名
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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
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简称
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Enasidenib
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别名
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AG-221, CC-90007, GTPL8960, CS-5017, AK431837
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中文名
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N/A
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化学式
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C19H17F6N7O
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分子量
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473.38
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CAS号
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1446502-11-9
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO100mg/ml; Ethanol100mg/ml
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溶液配制
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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。
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生物信息：
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产品描述
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Enasidenib is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme.
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信号通路
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Metabolism
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靶点
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IDH2
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－
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－
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－
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－
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IC50
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12nM
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－
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－
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－
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－
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体外研究
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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.
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体内研究
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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.
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临床实验
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N/A
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特征
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N/A
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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)：
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酶活性检测实验
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方法
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N/A
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细胞实验
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细胞系
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N/A
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浓度
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N/A
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处理时间
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N/A
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方法
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N/A
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动物实验
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动物模型
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Murine models of IDH2-mutant leukemia
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配制
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N/A
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剂量
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10mg/kg or 100mg/kg bid
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给药方式
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N/A
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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：
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产品编号
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产品名称
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包装
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SD7252-10mM
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Enasidenib (Dehydrogenase抑制剂)
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10mM×0.2ml
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SD7252-5mg
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Enasidenib (Dehydrogenase抑制剂)
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5mg
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SD7252-25mg
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Enasidenib (Dehydrogenase抑制剂)
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25mg
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—
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说明书
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1份
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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。
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