Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BAY-1436032 是一种选择性泛突变异柠檬酸脱氢酶 1 新型口服抑制剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 315 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,820 | 现货 | ||
50 mg | ¥ 4,250 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 788 | 现货 |
产品描述 | BAY-1436032 is a novel, selective and orally available inhibitor of pan-mutant isocitrate dehydrogenase 1 (IDH1). |
体外活性 | BAY-1436032 inhibits intracellular (R)-2-hydroxyglutarate (R-2HG) production in mouse hematopoietic cells expressing IDH1R132H or IDH1R132C (IC50s: 60 and 45?nM). R-2HG levels are not reduced in IDH2R140Q and IDH2R172K expressing mouse hematopoietic cells by BAY-1436032 at concentrations up to 10?μM. Colony growth is inhibited by 50% at a concentration of 0.1?μM BAY-1436032, while concentrations up to 100?μM do not suppress colony growth of patient-derived IDH1 wild-type AML cells. On morphologic evaluation myelomonocytic differentiation of myeloid progenitors is strongly induced by BAY-1436032. |
体内活性 | Long-term exposure to once-daily oral BAY-1436032 reveals nearly complete suppression of R-2HG production with 150?mg/kg BAY1436032. White blood cell counts constantly increase in vehicle-treated mice and, at a lower rate, in animals receiving 45?mg/kg BAY-1436032, while they remain constant in the 150?mg/kg cohort. Hemoglobin levels are slightly lower in the vehicle and 45?mg/kg groups as compared to the 150?mg/kg cohort at day 60, while platelet counts are significantly reduced in the vehicle and 45?mg/kg BAY-1436032 treated mice compared to the 150?mg/kg cohort at day 60. All mice receiving 150?mg/kg BAY-1436032 survive with minimal hCD45+ cell load in their peripheral blood until the end of observation at day 150 after treatment start, while vehicle-treated animals die from leukemia with a median survival of 91 days. Mice treated with 45?mg/kg BAY-1436032 display intermediate levels of CD14/CD15 expression. |
细胞实验 | Colony-forming cell (CFC) units are assayed in methylcellulose supplemented with 10?ng/mL IL-3, 10?ng/mL GM-CSF, 50?ng/ mL SCF, 50?ng/mL FLT3-ligand and 3?U/mL EPO. Vehicle or BAY-1436032 is added to methylcellulose containing 1 × 10^5 human mononuclear cells, which are plated in duplicate. Colonies are evaluated microscopically 10 to 14 days after plating by standard criteria. |
动物实验 | NSG mice are used and transplanted with primary acute myeloid leukemia (AML) cells from a patient with IDH1R132C mutant AML. Per condition 10 mice are treated with vehicle, 45 or 150?mg/kg body weight BAY-1436032 once daily by oral gavage for 150 days starting 17 days after transplantation. Finally, serum R-2HG levels and human CD45+ (hCD45+) cells are measured. |
分子量 | 489.53 |
分子式 | C26H30F3N3O3 |
CAS No. | 1803274-65-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 120 mg/mL (245.14 mM), sonification/heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0428 mL | 10.2139 mL | 20.4278 mL | 51.0694 mL |
5 mM | 0.4086 mL | 2.0428 mL | 4.0856 mL | 10.2139 mL | |
10 mM | 0.2043 mL | 1.0214 mL | 2.0428 mL | 5.1069 mL | |
20 mM | 0.1021 mL | 0.5107 mL | 1.0214 mL | 2.5535 mL | |
50 mM | 0.0409 mL | 0.2043 mL | 0.4086 mL | 1.0214 mL | |
100 mM | 0.0204 mL | 0.1021 mL | 0.2043 mL | 0.5107 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。
BAY-1436032 1803274-65-8 Metabolism Dehydrogenase Isocitrate Dehydrogenase (IDH) BAY 1436032 Inhibitor inhibit BAY1436032 inhibitor