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Flumatinib(HHGV678)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Flumatinib(HHGV678)图片
CAS NO:895519-90-1
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
Flumatinib (HHGV678) (HHGV678) 是一种口服的选择性 Bcr-Abl 抑制剂。 Flumatinib (HHGV678) 抑制 c-Abl，PDGFRβ；和 c-Kit，IC50 分别为 1.2 nM、307.6 nM 和 665.5 nM。
Cas No.895519-90-1
别名4-[(4-甲基-1-哌嗪基)甲基]-N-[6-甲基-5-[[4-(3-吡啶基)-2-嘧啶基]氨基]-3-吡啶基]-3-(三氟甲基)苯甲酰胺,HHGV678
Canonical SMILESO=C(NC1=CC(NC2=NC=CC(C3=CC=CN=C3)=N2)=C(C)N=C1)C4=CC=C(CN5CCN(C)CC5)C(C(F)(F)F)=C4
分子式C29H29F3N8O
分子量562.59
溶解度DMSO : ≥ 32 mg/mL (56.88 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Flumatinib (HHGV678) is a multi-kinase inhibitor with IC50 Values of 1.2 nM, 307.6 nM and 2662 nM for c-Abl, PDGFRβ and c-Kit respectively.

HH-GV-678 can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. In higher concentration, Flumatinib (HHGV678) can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell, however, Flumatinib (HHGV678) has no or little effect on other tyrosine kinase including EGFR, KDR, c-Src and HER2 [1]. Flumatinib (HHGV678) effectively overcame the drug resistance of certain KIT mutants with activation loop mutations (i.e., D820G, N822K, Y823D, and A829P) [2].

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 Flumatinib (HHGV678) 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 drug Flumatinib (HHGV678) was the main form recovered in human plasma, urine, and feces. The main metabolites of Flumatinib (HHGV678) in humans were the products of N-demethylation, N-oxidation, hydroxylation, and amide hydrolysis [3].

[1]. Luo H, et al. HH-GV-678, a novel selective inhibitor of Bcr-Abl, outperforms imatinib and effectively overrides imatinib resistance. Leukemia. 2010 Oct;24(10):1807-9. [2]. Zhao J, et al. Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants. Cancer Sci. 2013 Nov 10. [3]. Gong A, et al. Metabolism of flumatinib, a novel antineoplastic tyrosine kinase inhibitor, in chronic myelogenous leukemia patients. Drug Metab Dispos. 2010 Aug;38(8):1328-40.