Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Flumatinib (HHGV678) 是一种具有口服活性的选择性 Bcr-Abl 抑制剂,能够作用于 c-Abl (IC50:1.2 nM),PDGFRβ (IC50:307.6 nM) 和 c-Kit (IC50:665.5 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 248 | 现货 | ||
5 mg | ¥ 578 | 现货 | ||
10 mg | ¥ 747 | 现货 | ||
25 mg | ¥ 1,170 | 现货 | ||
50 mg | ¥ 1,580 | 现货 | ||
100 mg | ¥ 2,350 | 现货 | ||
200 mg | ¥ 3,490 | 现货 | ||
500 mg | ¥ 5,570 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 718 | 现货 |
产品描述 | Flumatinib (HHGV678) is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity. |
靶点活性 | c-Kit:2662 nM, PDGFRβ:307.6 nM, c-Abl:1.2 nM |
体外活性 | In higher concentration, HH-GV-678 can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell, however, HH-GV-678 has no or little effect on other tyrosine kinases including EGFR, KDR, c-Src and HER2. HH-GV-678 can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. Flumatinib effectively overcame the drug resistance of certain KIT mutants with activation loop mutations (i.e., D820 g, N822K, Y823D, and A829P). |
体内活性 | The purpose of this study was to identify the metabolites of flumatinib in CML patients, with the aim of determining the main metabolic pathways of lumatinib in humans after oral administration. Ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry revealed 34 metabolites; 7 primary metabolites were confirmed by comparison with synthetic reference standards. The results show that the parent drugflumatinib was the main form recovered in human plasma, urine, and feces. The main metabolites of flumatinib in humans were the products of N-demethylation, N-oxidation, hydroxylation, and amide hydrolysis |
别名 | HHGV678 |
分子量 | 562.59 |
分子式 | C29H29F3N8O |
CAS No. | 895519-90-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (88.87 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7775 mL | 8.8875 mL | 17.7749 mL | 44.4373 mL |
5 mM | 0.3555 mL | 1.7775 mL | 3.555 mL | 8.8875 mL | |
10 mM | 0.1777 mL | 0.8887 mL | 1.7775 mL | 4.4437 mL | |
20 mM | 0.0889 mL | 0.4444 mL | 0.8887 mL | 2.2219 mL | |
50 mM | 0.0355 mL | 0.1777 mL | 0.3555 mL | 0.8887 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。
Flumatinib 895519-90-1 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors PDGFR Bcr-Abl c-Kit Inhibitor HHGV 678 HHGV-678 inhibit Platelet-derived growth factor receptor HHGV678 CD117 SCFR inhibitor