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CHMFL-BMX-078

CHMFL-BMX-078

产品编号 T4268   CAS 1808288-51-8

CHMFL-BMX-078 是一种高效的、选择性的 II 型不可逆 BMX 激酶抑制剂,其 IC50=11 nM。

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CHMFL-BMX-078 Chemical Structure
CHMFL-BMX-078, CAS 1808288-51-8
规格 价格/CNY 货期 数量
1 mg ¥ 815 现货
5 mg ¥ 1,970 现货
10 mg ¥ 3,130 现货
25 mg ¥ 5,170 现货
50 mg ¥ 7,320 现货
100 mg ¥ 9,870 现货
1 mL * 10 mM (in DMSO) ¥ 2,730 现货
产品目录号及名称: CHMFL-BMX-078 (T4268)
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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 CHMFL-BMX-078 is a highly potent and selective type II irreversible BMX kinase inhibitor with an IC50 of 11 nM.
靶点活性 BMX kinase:11 nM.
体外活性 CHMFL-BMX-078 displays a high selectivity profile against the 468 kinases/mutants in the KINOMEscan evaluation and achieves at least 40-fold selectivity over BTK kinase (IC50=437 nM). For inactive state of BMX kinase, CHMFL-BMX-078 displays a binding Kd of 81 nM, while for the active state of BMX kinase, it exhibits a binding Kd of 10200 nM. CHMFL-BMX-078 exhibits antiproliferative effects against BaF3-TEL-BMX cells (GI50=0.016 μM) and selectivity over parental BaF3 cells. CHMFL-BMX-078 is about 80-fold more potent against BMX wt (EC50=5.8 nM) than C496S mutant (EC50=459 nM) for the inhibition of BMX total tyrosine phosphorylation.
体内活性 CHMFL-BMX-078 also displays an acceptable Cmax (13565.23 ng/mL) and AUC0-t (1386.41 ng/mL h) in iv injection. However, it is not absorbed by oral administration, indicating that this compound could be administrated through i.v. or i.p. injection when used as a research tool.
激酶实验 The kinase reaction system contains BMX or BTK, 1 μL of serially diluted CHMFL-BMX-078, and substrate Poly peptidewith 100 μM ATP. The reaction in each tube is started immediately by adding ATP and kept going for an hour under 37 °C. After the tube cooled for 5 min at room temperature, 5 μL solvent reactions are carried out in a 384-well plate. Then 5 μL of ADP-Glo reagent is added into each well to stop the reaction and consume the remaining ATP within 40 min. At the end, 10 μL of kinase detection reagent is added into the well and incubated for 30 min to produce a luminescence signal. Luminescence signal is measured with an automated plate reader.
动物实验 CHMFL-BMX-078 is dissolved in 55% saline containing 5% DMSO and 40% PEG400 by vortex. The final concentration of the stock solution is 1 mg/mL for administration.Rat: Six 8-week-old male Sprague?Dawley rats are fasted overnight before starting drug treatment via intravenous and oral administration. Animal blood collection time points are as follows. For groups 1, 3, and 5 (intravenous): 1 min, 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, and 8 h before and after administration is selected. For group 2, 4, and 6 (oral): 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, and 24 h before and after dosing. The plasma is collected for analysis.
分子量 625.67
分子式 C33H35N7O6
CAS No. 1808288-51-8

存储

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

溶解度

DMSO: 30 mg/mL (47.95 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 1 mM 1.5983 mL 7.9914 mL 15.9829 mL 39.9572 mL
5 mM 0.3197 mL 1.5983 mL 3.1966 mL 7.9914 mL
10 mM 0.1598 mL 0.7991 mL 1.5983 mL 3.9957 mL
20 mM 0.0799 mL 0.3996 mL 0.7991 mL 1.9979 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. Liang X, et al. Discovery of 2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a Highly Potent and Selective Type II Irreversible Bone Marrow Kinase in the X Chromosome (BMX) Kinase Inhibitor. J Med Chem. 2017 Mar 9;60(5):1793-1816.
zanubrutinib JAK3/BTK-IN-1 TL-895 DBt-10 Orelabrutinib Sunvozertinib QL-X-138 HCl BTK inhibitor 1

相关化合物库

该产品包含在如下化合物库中:
酪氨酸激酶分子库 抑制剂库 共价抑制剂库 激酶抑制剂库 NO PAINS 化合物库 已知活性化合物库 半胱氨酸共价化合物库 表型筛选靶点鉴定库 经典已知活性库 血管生成库

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

CHMFL-BMX-078 1808288-51-8 Angiogenesis Tyrosine Kinase/Adaptors BTK CHMFLBMX078 BMX Kinase inhibit CHMFL BMX 078 CHMFL-BMX 078 Inhibitor CHMFL-BMX078 inhibitor

 

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