Flumatinib

99.90%

Flumatinib

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品牌：源叶(MedMol)

产品编号：S87120 一键复制产品信息

CAS号：895519-90-1

分子式：C₂₉H₂₉F₃N₈O

分子量：562.5887

别名：HHGV678；氟马替尼

货号	规格	价格	上海	北京	珠海	重庆	武汉
S87120-5mg	99.90%	￥400.00 S87120-5mg ￥400.00 现货	2 2	-	-	-	-
S87120-10mg	99.90%	￥600.00 S87120-10mg ￥600.00 现货	5 5	-	-	-	-
S87120-50mg	99.90%	￥1280.00 S87120-50mg ￥1280.00 现货	3 3	-	-	-	-
S87120-200mg	≥99%	￥3320.00 S87120-200mg ￥3320.00 2-3天	0 货期：2-3天	-	-	-	-

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产品介绍参考文献(1篇) 质检证书(COA) 摩尔浓度计算器相关产品

产品描述：

Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively

靶点：

IC50 Value: 1.2 nM (c-Abl); 307.6 nM(PDGFRβ); 2662 nM (c-Kit);Bcr-Abl;PDGFR;c-Kit

体外研究：

Flumatinib (HH-GV-678) can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. In higher concentration, Flumatinib can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell, however, Flumatinib 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)。

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.777 ml	8.887 ml	17.775 ml
5 mM	0.355 ml	1.777 ml	3.555 ml
10 mM	0.178 ml	0.889 ml	1.777 ml
50 mM	0.036 ml	0.178 ml	0.355 ml