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• 产品描述： R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kd values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50 of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence

• 靶点： KDR:10 nM (IC50);FGFR1:28 nM (IC50);VEGFR;FGFR;FLT;PDGFR

• 体内研究：
  R1530 (1.56, 25, and 50 mg/kg; p.o.; daily, for 28 days.) has notable antitumor activity across a broad range of human xenograft models, with minimal toxicity. Animal Model: Human tumor xenograft models Dosage: 1.56, 25 and 50 mg/kg Administration: Oral administration; daily, for 28 days. Result: Inhibited tumor growth in all models, with regression observed in all models tested at a 50 mg/kg dose.

• 参考文献：
  1. Jin-Jun Liu, et al. Discovery of a Highly Potent, Orally Active Mitosis/Angiogenesis Inhibitor R1530 for the Treatment of Solid Tumors. ACS Med Chem Lett. 2013 Feb 14; 4(2): 259–263. 2. Christian Tovar, et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle. 2010 Aug 15;9(16):3364-75.

• 溶解性： Soluble  in  DMSO

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.803 ml	14.014 ml	28.028 ml
  5 mM	0.561 ml	2.803 ml	5.606 ml
  10 mM	0.28 ml	1.401 ml	2.803 ml
  50 mM	0.056 ml	0.28 ml	0.561 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 *