Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Enasidenib (AG-221) 是口服具有活力的、可逆的、选择性IDH2突变酶抑制剂,抑制IDH2R140Q 和 IDH2R172K 的IC50分别为100 和 400 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 243 | 现货 | ||
2 mg | ¥ 339 | 现货 | ||
5 mg | ¥ 529 | 现货 | ||
10 mg | ¥ 763 | 现货 | ||
25 mg | ¥ 1,370 | 现货 | ||
50 mg | ¥ 2,320 | 现货 | ||
100 mg | ¥ 3,490 | 现货 | ||
200 mg | ¥ 4,970 | 现货 | ||
500 mg | ¥ 7,580 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 593 | 现货 |
产品描述 | Enasidenib (AG-221) is an orally available inhibitor of specific mutant forms of the mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity. |
靶点活性 | IDH2R172K:400 nM, IDH2R140Q:100nM |
体外活性 | The compound has been demonstrated to reduce 2-HG levels by >90% and reverse histone and deoxyribonucleic acid (DNA) hypermethylation in vitro, and to induce differentiation in leukemia cell models[2]. |
体内活性 | AG-221 is able to potently reduce 2HG found in the bone marrow, plasma and urine of engrafted mice. Treatment also induced a dose dependent, statistically significant, survival benefit. A proliferative burst of the human specific CD45+ blast cells is followed by cellular differentiation as measured by the expression of CD11b, CD14 and CD15 and cell morphology after AG-221 treatment[2]. AG-221 treatment also restores megakaryocyte-erythroid progenitor (MEP) differentiation that is suppressed by mutant IDH2 expression and reverses the effects of mutant IDH2 on DNA methylation in mutant stem/progenitor cells. Clinicalal trials combining IDH2 inhibitors with other targeted AML therapies are warranted in order to increase therapeutic efficacy[1]. |
激酶实验 | Untranslated region-mediated luciferase reporter expression: HEK293 cells are transfected with a GEMS reporter vector that contains the luciferase open-reading frame flanked by and under post-transcriptional control of the BMI-1 5′ and 3′ UTRs. The resulting stable cells (F8) are treated with PTC-209 or vehicle control overnight, and then luciferase reporter activity is determined using Bright-Glo assays. The assays are run in triplicate for each point, and the percentage of inhibition was calculated against vehicle control. |
别名 | 恩西地平, AG-221 |
分子量 | 473.38 |
分子式 | C19H17F6N7O |
CAS No. | 1446502-11-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 100 mg/mL (211.25 mM)
DMSO: 50 mg/mL (105.62 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.1125 mL | 10.5623 mL | 21.1247 mL | 52.8117 mL |
5 mM | 0.4225 mL | 2.1125 mL | 4.2249 mL | 10.5623 mL | |
10 mM | 0.2112 mL | 1.0562 mL | 2.1125 mL | 5.2812 mL | |
20 mM | 0.1056 mL | 0.5281 mL | 1.0562 mL | 2.6406 mL | |
50 mM | 0.0422 mL | 0.2112 mL | 0.4225 mL | 1.0562 mL | |
100 mM | 0.0211 mL | 0.1056 mL | 0.2112 mL | 0.5281 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。
Enasidenib 1446502-11-9 Metabolism Dehydrogenase Isocitrate Dehydrogenase (IDH) AG 221 inhibit AG221 恩西地平 Inhibitor AG-221 inhibitor