化合物Flumatinib T4320

Product Introduction
Bioactivity


英文名: Flumatinib

描述: 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)。

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

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

溶解度: DMSO : 50 mg/mL (88.87 mM)


关键字: Inhibitor | HHGV 678 | HHGV-678 | Bcr-Abl | inhibit | Platelet-derived growth factor receptor | Flumatinib | PDGFR | CD117 | SCFR | c-Kit

相关产品: Olverembatinib | GNF-7 | CpCDPK1/TgCDPK1-IN-1 | Dasatinib monohydrate | AT9283 | Nilotinib | BCR-ABL-IN-8 | PP1 | Gypsogenin | Dasatinib

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Approved Drug Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途