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AGI-6780

AGI-6780

产品编号 T1809   CAS 1432660-47-3

AGI6780 能够选择性抑制肿瘤相关突变体IDH2R140Q,IC50=23±1.7 nM。它对IDH2WT 的作用效果微弱,IC50=190±8.1 nM。

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AGI-6780 Chemical Structure
AGI-6780, CAS 1432660-47-3
规格 价格/CNY 货期 数量
1 mg ¥ 279 现货
2 mg ¥ 398 现货
5 mg ¥ 655 现货
10 mg ¥ 1,270 现货
25 mg ¥ 2,070 现货
50 mg ¥ 3,230 现货
100 mg ¥ 4,630 现货
500 mg ¥ 9,630 现货
1 mL * 10 mM (in DMSO) ¥ 717 现货
产品目录号及名称: AGI-6780 (T1809)
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纯度: 98.15%
纯度: 97.47%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant.
靶点活性 IDH2 R140Q mutant:23 nM
体内活性 AGI-6780逆转TF-1细胞中IDH2/ R140Q诱导的分化阻滞,并诱导原发性人类IDH2/R140Q AML患者样品中的急剧分化。AGI-6780有效降低异位过表达IDH2/R140Q的细胞系中的(R)-2-羟基戊二酸(2 hG)水平,EC 50为20 nM,与其他脱氢酶相比,具有优异的选择性。
激酶实验 AGI-6780 is prepared as 10 mM stock in DMSO and diluted to 50X final concentration in DMSO, for a 50 μL reaction mixture. IDH enzyme activity converting alpha-ketoglutarate to 2-hydroxyglutarate is measured using a NADPH depletion assay. In the assay the remaining cofactor is measured at the end of the reaction with the addition of a catalytic excess of diaphorase and resazurin, to generate a fluorescent signal in proportion to the amount of NADPH remaining. IDH enzyme activity in the direction of isocitrate to alpha-ketoglutarate conversion is measured by direct coupling of the NADPH production to conversion of resazurin to resorufin by diaphorase. In both cases, resorufin is measured fluorometrically at Ex544 Em590[1].
细胞实验 AGI-6780 is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. Cells are sorted from fresh or frozen bone marrow aspirates and blood samples after labelling with PE-CD34, APC-CD38, PE-CD14, FITC-CD3 (clone HIT3a) and PECy7-CD19 (clone SJ25C1) antibodies using a MoFlow cell sorter. Unfractionated nucleated blood or bone marrow cells are plated in Methocult H4434 methylcellulose medium at 104 cells/dish, in duplicate dishes per condition. AGI-6780 (5 mM) is directly added to the medium. Dishes are incubated in a humidified incubator at 37°C and colonies containing at least 30 cells are counted after 13 days[1].
分子量 481.51
分子式 C21H18F3N3O3S2
CAS No. 1432660-47-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 89 mg/mL (184.8 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 89 mg/mL (184.8 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.0768 mL 10.384 mL 20.768 mL 51.92 mL
5 mM 0.4154 mL 2.0768 mL 4.1536 mL 10.384 mL
10 mM 0.2077 mL 1.0384 mL 2.0768 mL 5.192 mL
20 mM 0.1038 mL 0.5192 mL 1.0384 mL 2.596 mL
50 mM 0.0415 mL 0.2077 mL 0.4154 mL 1.0384 mL
100 mM 0.0208 mL 0.1038 mL 0.2077 mL 0.5192 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Wang F, et al. Science. 2013, 340(6132), 622-666. 2. Chen J, Yang J, Wei Q, et al. Cell Communication and Signaling. 2020, 18(1): 1-12. 3. Chen J, Yang J, Wei Q, et al. Identification of a selective inhibitor of IDH2/R140Q enzyme that induces cellular differentiation in leukemia cells[J]. Cell Communication and Signaling. 2020, 18: 1-12. 4. Chen J, Yang J, Wei Q, et al. Identification of a selective inhibitor of IDH2/R140Q enzyme that induces cellular differentiation in leukemia cells[J]. Cell Communication and Signaling . 2020, 18: 1-12.

文献引用

1. Chen J, Yang J, Wei Q, et al. Identification of a selective inhibitor of IDH2/R140Q enzyme that induces cellular differentiation in leukemia cells. Cell Communication and Signaling. 2020, 18(1): 1-12 2. Tan Q, Zhang X, Li S, et al.DMT1 differentially regulates mitochondrial complex activities to reduce glutathione loss and mitigate ferroptosis.Free Radical Biology and Medicine.2023 3. Yang J, Chen J, Chang J, et al.IDH2/R140Q mutation confers cytokine-independent proliferation of TF-1 cells by activating constitutive STAT3/5 phosphorylation.Cell Communication and Signaling.2024, 22(1): 116.
LDHA-IN-4 4-Hydroxynonenal Galloflavin 3-Hydroxybenzaldehyde PKUMDL-WQ-2101 Tenuifoliside C Benzyl alcohol ML390

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 抗癌活性化合物库 抗癌化合物库 抗代谢疾病化合物库 代谢化合物库 抗癌细胞代谢库 脂代谢化合物库 含氟化合物库 共价抑制剂库 NO PAINS 化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

AGI-6780 1432660-47-3 Metabolism Dehydrogenase Isocitrate Dehydrogenase (IDH) inhibit AGI6780 Inhibitor AGI 6780 inhibitor

 

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