Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 89 mg/mL (184.8 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 89 mg/mL (184.8 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
AGI-6780 1432660-47-3 Metabolism Dehydrogenase Isocitrate Dehydrogenase (IDH) inhibit AGI6780 Inhibitor AGI 6780 inhibitor