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AGI-6780

品牌
Sigma-Aldrich
CAS
1432660-47-3
货号
SML0895
规格纯度
≥98% (HPLC)
参考价格
1746.67 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

包装

5, 25 mg in glass bottle

生化/生理作用

AGI-6780 is a selective inhibitor of IDH2/R140Q a tumor-associated mutant of isocitrate dehydrogenase IDH2. Several human cancers have somatic point mutations in the genes encoding isocitrate dehydrogenases 1 and 2 (IDH1 and IDH2), confering a gain-of-function in cancer cells in which the mutant enzymes produce the oncometabolite (R)-2-hydroxyglutarate, [(R)-2HG]. (R)-2HG inhibits histone- and DNA-modifying enzymes, resulting in altered gene expression, histone and DNA hypermethylation, and inducing a block in cellular differentiation that promotes tumorigenesis. AGI-6780 reduced (R)-2HG levels in cell lines overexpressing IDH2/R140Q with an EC50 of 20 nM, and induced differentiation of TF-1 erythroleukemia and primary human acute myelogenous leukemia cells in vitro. AGI-6780 binds allosterically at the dimer interface of IDH2. AGI-6780 shows good selectivity against other dehydrogenases, including the closely related IDH1-WT or R132H mutant enzymes.

特点和优势

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基本信息

经验(实验)分子式C21H18F3N3O3S2
分子量481.51
NACRESNA.77

产品性质

质量水平100
测定≥98% (HPLC)
形式powder
颜色 white to light brown
溶解性DMSO: 20 mg/mL, clear
储存温度2-8℃

安全信息

储存分类代码13 - Non Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

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