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• 产品描述： CEP-37440 is a potent, orally active dual FAK/ALK inhibitor with IC50 values of 2.3 nM and 3.5 nM for FAK and ALK, respectively. CEP-37440 decreases the cell proliferation by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397)

• 靶点： IC50:2.3 nM (FAK) and 3.5 nM (ALK);FAK; ALK

• 体外研究：
  CEP-37440 (0-3000 nM; 0-192 h) decreases the proliferation of inflammatory breast cancer (IBC) cells in a dose-dependent manner. CEP-37440 (1000 nM; 0-120 h) decreases phospho-FAK1 (Tyr 397) and maintains its low level over time in FC-IBC02, SUM 190, and KPL4. CEP-37440 (0-3000 nM; Sup-M2 and Karpas-299 cells) induces proapoptotic caspases in a dose-dependent manner. Cell Viability Assay Cell Line: FC-IBC02, KPL4, SUM190, MDA-IBC03 and SUM149 cells Concentration: 0, 300, 1000, 2000 and 3000 nM Incubation Time: 0, 24, 48, 72, 96, 120, 144, 168, and 192 hours Result: Reduced the proliferation of three out of five IBC cell lines at low concentration. Inhibited the proliferation almost completely at 3000 nM concentration. Western Blot Analysis Cell Line: FC-IBC02, SUM 190, and KPL4 cells Concentration: 1000 nM Incubation Time: 0, 48, 72, 96 and 120 hours Result: Decreased phospho-FAK1 by half in FC-IBC02, SUM190, and KPL4 cells after 48 hours.

• 体内研究：
  CEP-37440 (3-55 mg/kg; p.o.; b.i.d and q.d., for 12 d) inhibits breast tumor growth in Sup-M2 xenograftin SCID mice. CEP-37440 (30 mg/kg; p.o; once, for 24 h) inhibits tyrosine phosphorylation in Sup-M2 xenografts mice. CEP-37440 (55 mg/kg; p.o; once, for 24 h) inhibits FAK phosphorylation in CWR22 xenografts in Nude mice. CEP-37440 (1-10 mg/kg; p.o and i.v.; CD-1 mouse, Sprague-Dawley (SD) rats) has good pharmacokinetic parameters. Animal Model: SCID/Beige with Sup-M2 xenografts Dosage: 3 mg/kg (b.i.d), 10 mg/kg (b.i.d), 30 mg/kg (b.i.d and q.d. ), and 55 mg/kg (q.d.) Administration: Oral administration; b.i.d and q.d., for 12 days Result: Inhibited tumor growth in a dose-dependent manner.

• 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	1.724 ml	8.619 ml	17.238 ml
  5 mM	0.345 ml	1.724 ml	3.448 ml
  10 mM	0.172 ml	0.862 ml	1.724 ml
  50 mM	0.034 ml	0.172 ml	0.345 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 *