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• 产品描述： A939572 是一种有效的、口服生物可利用的 stearoyl-CoA desaturase1 (SCD1) 的抑制剂，对 mSCD1 和 hSCD1 的 IC50值分别为 <4 nM 和 37 nM

• 靶点： mSCD1(Cell-free assay):4 nM; hSCD1(Cell-free assay):37 nM;Dehydrogenase; Stearoyl-CoADesaturase(SCD)

• 体外研究：
  A939572 demonstrates a significant dose-dependent decrease in proliferation in Caki1, A498, Caki2, and ACHN at day 5. In congruity with previous experimentation examining SCD1 lentiviral knockdown models, A939572 induces apoptosis confirmed by PARP cleavage via western blot analysis in all four cell lines. Treatment of ccRCC cells with A939572 induces Endoplasmic Reticulum Stress

• 体内研究：
  When compared to the placebo control, all treatment groups (A939572, Tem, and Combo) exhibits decreased proliferation as marked by reduction in percent positivity of nuclear Ki67 staining, with the combinatorial group demonstrating the most significant decline. Combinatorial application of A939572 with temsirolimus synergistically inhibits tumor growth in vivo

• 细胞实验： Cell lines: Caki1, A498, Caki2, ACHN ccRCC cells Concentrations: 75 nM Incubation Time: 24 h Method: In order to determine the mechanism of decreased proliferation and induction of cell death associated with loss of SCD1 activity in ccRCC cells, gene array analysis was performed with Caki1, A498, Caki2, and ACHN ccRCC cells treated for 24 hours with a 75nM dose of A939572 compared to DMSO control.

• 动物实验： Animal Models: athymic nu/nu mice Dosages: 30 mg/kg Administration: Oral gavage

• 参考文献：
  1. Zhili Xin, et al. Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4298-302. 2. Christina A von Roemeling, et al. Stearoyl-CoA desaturase 1 is a novel molecular therapeutic target for clear cell renal cell carcinoma. Clin Cancer Res. 2013 May 1;19(9):2368-80.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.578 ml	12.891 ml	25.782 ml
  5 mM	0.516 ml	2.578 ml	5.156 ml
  10 mM	0.258 ml	1.289 ml	2.578 ml
  50 mM	0.052 ml	0.258 ml	0.516 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 *