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• 产品描述： ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

• 靶点： Aurora A：14 nM (IC50)；KDR：58.2 nM (IC50)；Flt-4：15.9 nM (IC50)；FGFR1：92.7 nM (IC50)；FGFR2：70.8 nM (IC50)；PDGFRα：56.4 nM (IC50)；Flt3：1.86 nM (IC50);Apoptosis; VEGFR; FGFR; FLT; c-RET; PDGFR; Src; AuroraKinase

• 体内研究：
  ENMD-2076 treatment results in statistically significant, dose dependent inhibition of tumor growth or tumor regression. Moreover, there is no correlation between tumor growth rate and antitumor efficacy, which would conceivably be expected for a mitotic kinase inhibitor, as fast growing (e.g., A375 melanoma) and slow-growing (e.g., HT29 colon carcinoma) tumors are similarly inhibited by ENMD-2076. ENMD-2076 is well tolerated at daily doses up to 302 mg/kg (equivalent to 200 mg/kg of the free base), with no weight loss or signs of morbidity noted in any study at this dose with the exception of the A375 model

• 参考文献：
  1. Fletcher GC, et al. ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action. Mol Cancer Ther. 2011 Jan;10(1):126-37. 2. Wang X, et al. Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD-2076, against multiple myeloma. Br J Haematol. 2010 Aug;150(3):313-25.

• 溶解性： DMSO  :  ≥  31  mg/mL  (82.56  mM)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.663 ml	13.317 ml	26.633 ml
  5 mM	0.533 ml	2.663 ml	5.327 ml
  10 mM	0.266 ml	1.332 ml	2.663 ml
  50 mM	0.053 ml	0.266 ml	0.533 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 *