计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥98% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
(S,R)-WT IDH1 Inhibitor 2 (GSK321) is a potent, selective mutant IDH1 inhibitor with IC 50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1 , respectively, and >100-fold selectivity over IDH2. (S,R)-WT IDH1 Inhibitor 2 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-WT IDH1 Inhibitor 2 can be used for research of acute myeloid leukemia (AML) and other cancers
In Vitro
(S,R)-WT IDH1 Inhibitor 2 (GSK321; 0.1-10000 nM; 24 h) inhibits intracellular 2-HG production in HT1080 cells with an EC 50 value of 85 nM. (S,R)-WT IDH1 Inhibitor 2 (0-5 μM; 48 h; HT1080 fibrosarcoma cells) leads to reduction of histone H3K9 dimethylation (H3K9me2). (S,R)-WT IDH1 Inhibitor 2 (3 μM; 22 d) decreases intracellular 2-HG in a dose-dependent manner (R132G, 0.13-fold; R132C, 0.15-fold; R132H, 0.29-fold). (S,R)-WT IDH1 Inhibitor 2 (3 μM; 15 d) affects proliferation of primary IDH1 mutant AML cells. (S,R)-WT IDH1 Inhibitor 2 (3 μM; 9 d) induces differentiation in primary IDH1 mutant AML blasts and immature stem-like cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: IDH1 mutant AML cells Concentration: 3 μM Incubation Time: 15 days Result: Increased in cell numbers (2-fold to 15-fold) in IDH1 mutant AML cells. Cell Cycle AnalysisCell Line: IDH1 mutant AML cells Concentration: 3 μM Incubation Time: 15 days Result: Decreased in quiescent (G0)-phase cells and increased in G1-phase in R132G IDH1. Western Blot AnalysisCell Line: HT1080 fibrosarcoma cells Concentration: 0, 0.5 and 5 μM Incubation Time: 48 hours Result: Induced markedly decreased H3K9me2 levels.
In Vivo
(S,R)-WT IDH1 Inhibitor 2 (GSK321; 150 mg/kg; i.p.; daily, for 15 d; male CD-1 mice with IDH1 mutant AML xenograft) reduces leukemic blasts in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male CD-1 mice with IDH1 mutant AML xenograft Dosage: 150 mg/kg Administration: Intraperitoneal injection; daily, for 15 days Result: Decreased in 2HG in IDH1-mutant AML cells. Decreased in the percentage of blast cells ( SSClow CD45 low/+ ) and a relative increase in mature lymphoid and granulocytic/monocytic cells.
Form:Solid
IC50& Target:IDH1
规格
规格或纯度
≥98%
英文名称
(S,R)-GSK321
生化机理
(S,R)-WT IDH1 抑制剂 2 (GSK321) 是一种强效的选择性突变 IDH1 抑制剂，对 R132G、R132C、R132H 和 WT IDH1 的 IC 50 值分别为 2.9、3.8、4.6 和 46 nM，对 IDH2 的选择性大于 100 倍。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥98%
名称和识别符
分子类型
小分子
分子量
501.55
技术文档
高级数据
质检证书（CoA,COO,BSE/TSE 和分析图谱)
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溶液计算器
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