首页 工具
登录
购物车
BAY-1436032

BAY-1436032

产品编号 TQ0042   CAS 1803274-65-8

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。

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
BAY-1436032 Chemical Structure
BAY-1436032, CAS 1803274-65-8
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
产品目录号及名称: BAY-1436032 (TQ0042)
点击图片重新获取验证码
选择批次  
纯度: 99.65%
纯度: 99.38%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

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

溶解度

DMSO: 120 mg/mL (245.14 mM), sonification/heating is recommended.

溶液配制表

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

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
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Chaturvedi A, et al. Pan-mutant-IDH1 inhibitor BAY1436032 is highly effective against human IDH1 mutant acute myeloid leukemia in vivo. Leukemia. 2017 Oct;31(10):2020-2028.
Orotic acid IDH-305 alpha-Mangostin DHODH-IN-16 DHODH-IN-17 CB29 11β-HSD1 inibitor 17 Vidofludimus

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌临床化合物库 抗癌活性化合物库 已知活性化合物库 抑制剂库 谷氨酰胺代谢化合物库 药物功能重定位化合物库 经典已知活性库 NO PAINS 化合物库 代谢化合物库

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
%
% 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

BAY-1436032 1803274-65-8 Metabolism Dehydrogenase Isocitrate Dehydrogenase (IDH) BAY 1436032 Inhibitor inhibit BAY1436032 inhibitor

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼