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• 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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

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

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *