• 产品描述： KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities

• 靶点： PDGFRβ:520 nM (Kd);PDGFRα:300 nM (Kd);B-Raf;c-Raf;FLT3:52 nM (Kd);KIT:170 nM (Kd);Raf; FLT; PDGFR; c-Kit

• 体外研究：
  KG5 (Compound 6) inhibits vascular smooth muscle cells (VSMCs) and endothelial cells viability with EC50 values of 0.59 μM and 0.54 μM, respectively. Compound 6 selectively blocks S338 phosphorylation, yet does not influence S259. KG5 (Compound 6) inhibits only PDGFRα and β with Kds of 300 and 520 nM, respectively, and Flt3 and KIT at 52 and 170 nM, respectively. KG5 (Compound 6; 5 μM) inhibits phosphorylation of MEK and ERK in endothelial cells stimulated with bFGF or VEGF

• 体内研究：
  KG5 (Compound 6; 100 mg/kg; oral administration; daily; for 26 days) treatment prevents tumor growth in an orthotopic renal cell carcinoma model. KG5 (Compound 6; 50 mg/kg; i.p.; twice daily) treatment completely blocks angiogenesis relative to vehicle control in mice (injected with Matrigel containing bFGF). Pharmacokinetic analysis of the dose and formulation of KG5 used indicated a Cmax of 3.6 μg/mL, T1/2 of 11.5 h, and an area under the concentration time curve (AUC0-12h) of 14.7 μg•h/mL. KG5 (Compound 6; 1 μM) disrupts a late step in angiogenesis during zebrafish embryogenesis. Animal Model: Male Nu/Nu mice injected with SN12C-RFP cells Dosage: 100 mg/kg Administration: Oral administration; daily; for 26 days Result: Prevented tumor growth in an orthotopic renal cell carcinoma model.

• 参考文献：
  1. Eric A Murphy, et al. Disruption of angiogenesis and tumor growth with an orally active drug that stabilizes the inactive state of PDGFRbeta/B-RAF. Proc Natl Acad Sci U S A. 2010 Mar 2;107(9):4299-304.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.177 ml	10.883 ml	21.765 ml
  5 mM	0.435 ml	2.177 ml	4.353 ml
  10 mM	0.218 ml	1.088 ml	2.177 ml
  50 mM	0.044 ml	0.218 ml	0.435 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 *