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位置: 首页> 品牌> Sigma-Aldrich> IDH2 Inhibitor, R140Q Somatic Mutant-Specific, AGI-6780-CAS 1432660-47-3-Calbiochem

IDH2 Inhibitor, R140Q Somatic Mutant-Specific, AGI-6780-CAS 1432660-47-3-Calbiochem

品牌
Sigma-Aldrich
CAS
1432660-47-3
货号
5.09880
规格纯度
A cell-permeable inhibitor of isocitrate dehydrogenase 2 R140Q mutant-containing dimers. Has minimal effect on wild type dimer-catalyzed alpha-KG production.
价格
2579.1 *本价格含增值税费
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半岛bd体育手机客户端 名称:
1432660-47-3
IDH2 Inhibitor, R140Q Somatic Mutant-Specific, AGI-6780-CAS 1432660-47-3-Calbiochem
Isocitrate Dehydrogenase 2 R140 Somatic Mutant Inhibitor, AGI6780
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

一般描述

A cell-permeable ureido-benzenesulfonamide that inhibits α-ketoglutarate (α-KG)-to-(R)-2-hydroxyglutarate (2-HG) conversion catalyzed by Isocitrate Dehydrogenase-2 (IDH2) R140Q mutant-containing dimers (IC50/preincubation time = 4 nM/16 h & 120 nM/1 h against R140Q-wt heterodimer; 23 nM/16 h & 170 nM/1 h against R140Q homodimer) in a substrate-non-competitive and NADPH-uncompetitive manner by targeting the dimer interface via a high affinity allosteric interaction with a slow-binding kinetic (kon= 5.8 x 104/M/min;koff= 8.3 x 10-3/min) and stabilizing the mutant dimers in an inactive conformation, while displaying much reduced potency against wt IDH2 dimer-catalyzed α-KG production (IC50/preincubation time = 190 nM/16 h & 2.7 ?M/1 h) and little or no activity toward LDHA, 3PGDH, GDH, G6PDH, R132H mutant or wt IDH1. Selectively inhibits 2-HG production in R140Q IDH2-expressing U87 glioblastoma & TF-1 erythroleukemia, but not R132H-expressing U87 cultures (IC50in 48 h = 11 nM, 18 nM, and >100 ?M, respectively) and sensitizes R140Q IDH2-expressing TF-1 to EPO-induced erythroid differentiation. Likewise, inhibition of 2-HG production in primary bone marrow cultures from AML patients with R140Q mutation (complete inhibition with 5 ?M AGI-6780) is shown to reactivate the differentiation of immature AML blasts without cytotoxicity. IDH1 Inhibitor, R132 Somatic Mutant-Specific, AGI-5198 (>Cat. No. 410972) is also available.
A cell-permeable urea sulfonamide that inhibits the activity of Isocitrate Dehydrogenase 2 (IDH2) R140Q mutant-containing dimers in an α-ketoglutarate/α-KG-non-competitive and NADPH-uncompetitive manner by stabilizing the mutant dimers in an inactive conformation via a high-affinity allosteric interaction at the dimer interface with a slow-binding kinetic (kon= 5.8 x 104/M/min;koff= 8.3 x 10-3/min), while displaying much reduced potency against wt IDH2 dimer-catalyzed α-KG production and little or no activity toward wt IDH1 or R132H IDH2 mutant. Selectively inhibits 2-HG production in IDH2 R140Q, but not R132H, mutant-expressing U87 cultures (IC50in 48 h = 11 nM vs. >100 ?M). AGI-6780 treatment (5 ?M) of primary bone marrow cultures from AML patients with R140Q mutation is shown to reactivate the differentiation of immature AML blasts without cytotoxicity.

生化/生理作用

Cell permeable: yes
Reversible: yes
Target IC50: 4 nM/16 h & 120 nM/1 h against R140Q-wt heterodimer
Primary Target
(IDH2) R140Q mutants

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他说明

Wang, F., et al. 2013.Science340,622.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式 C21H18F3N3O3S2
分子量 481.51

半岛bd体育手机客户端 性质

质量水平 100
测定 ≥95% (HPLC)
形式 powder
manufacturer/tradename Calbiochem?
储存条件 OK to freeze
protect from light
颜色 off-white
溶解性 DMSO: 100 mg/mL
储存温度 2-8℃

安全信息

储存分类代码 11 - Combustible Solids
WGK WGK 3
闪点(F) Not applicable
闪点(C) Not applicable

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