货号	规格	价格	上海	北京	珠海	重庆	武汉
S87121-1mg	≥99%	￥330.00 S87121-1mg ￥330.00 3-5天	0 货期：3-5天	-	-	-	-
S87121-5mg	≥99%	￥820.00 S87121-5mg ￥820.00 3-5天	0 货期：3-5天	-	-	-	-
S87121-500mg	≥99%	￥14500.00 S87121-500mg ￥14500.00 3-5天	0 货期：3-5天	-	-	-	-

大包装询价收藏产品

加入购物车

到货通知，提交手机号入库后将短信通知。

产品描述：

Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model

靶点：

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

体外研究：

Flumatinib mesylate (HH-GV-678) (0-1000 μM; 4, 7 and 10 days) blocks cellular Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation in K562 leukemia cells. Flumatinib mesylate (HH-GV-678) (0-10 μM; 72 hours) remarkably decreases the number of cells in chronic myelogenous leukemia cell lines. Cell Proliferation Assay Cell Line: Chronic myelogenous leukemia cell line Concentration: 0-10 μM Incubation Time: 72 hours Result: The proliferation inhibitory activity was 32-to 58-fold more potent than that of imatinib and 2-to 5-fold more potent than that of nilotinib. Western Blot Analysis Cell Line: K562 cells Concentration: 0, 1, 3, 10, 30, 100, 300 and 1000 μM Incubation Time: 4, 7 and 10 days Result: Suppressed cellular Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation.

体内研究：

Flumatinib mesylate (HH-GV-678) (18-75 mg/kg; p.o.; Twice daily, for 14 days.) inhibits tumor growth in nude mice. Animal Model: Nude mice (subcutaneously injecting K562 cells) Dosage: 18.75, 37.5, 75 mg/kg Administration: Oral administration; Twice daily, for 14 days. Result: Inhibited the growth of K562 xenografts in a dose-dependent manner and induced regression in all tumors at a daily dose of 75 mg/kg for nine days.

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.

溶解性：

Soluble in DMSO、H2O

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.518 ml	7.591 ml	15.182 ml
5 mM	0.304 ml	1.518 ml	3.036 ml
10 mM	0.152 ml	0.759 ml	1.518 ml
50 mM	0.03 ml	0.152 ml	0.304 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

质检证书(COA)

输入产品批号：

如何获取质检证书(COA)?

请输入货号和一个与之匹配的批号。
例如:
批号：JS298415 货号：S20001-25g
在货品标签上如何找到货号和批号?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

Flumatinib (mesylate)