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• 產(chǎn)品描述： A939572 是一種有效的、口服生物可利用的 stearoyl-CoA desaturase1 (SCD1) 的抑制劑，對(duì) mSCD1 和 hSCD1 的 IC50值分別為 <4 nM 和 37 nM

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

• 體外研究：
  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

• 體內(nèi)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

• 細(xì)胞實(shí)驗(yàn)： 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.

• 動(dòng)物實(shí)驗(yàn)： Animal Models: athymic nu/nu mice Dosages: 30 mg/kg Administration: Oral gavage

• 參考文獻(xiàn)：
  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

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	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

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶(hù)參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *