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• 產(chǎn)品描述： AZ20 is an effective and specific inhibitor of ATR kinase (IC50: 5 nM, in a cell-free assay), 8-fold selectivity over mTOR

• 靶點(diǎn)： mTOR;ATM/ATR;ATM/ATR;?mTOR

• 體外研究：
  AZ20（10 μM）可使CYP3A4介導(dǎo)的咪達(dá)唑侖代謝的50％被抑制.LoVo腫瘤的雌性裸鼠中,服用13天AZ20（25 mg/kg,2次/天,p.o.;50 mg/kg/day,p.o. ）可使腫瘤生長(zhǎng)受到顯著抑制,這與異種移植組織中γH2AX核染色的持續(xù)廣泛升高有關(guān)

• 體內(nèi)研究：
  在體外,AZ20濃度依賴性地降低pChk1 Ser345/317/296水平。延長(zhǎng)AZ20的處理時(shí)間可增加γH2AX核染色,這是因?yàn)榇嬖趶?fù)制壓力,且與S期阻滯和組蛋白H3的磷酸化水平增加有關(guān)。AZ20對(duì)體外生長(zhǎng)抑制和細(xì)胞死亡的誘導(dǎo)作用是完全不同于其它細(xì)胞毒性藥物的。AZ2與ATM 抑制劑KU-60019聯(lián)用會(huì)增加細(xì)胞毒性

• 細(xì)胞實(shí)驗(yàn)： AZ20 is dissolved in 100% DMSO. Compound dose ranges are created by diluting in 100% DMSO and then further into assay medium (EMEM, 10% FCS, 1% glutamine) using a Labcyte Echo acoustic dispensing instrument. Cells are plated in 384-well Costar plates at 9×104 cells per mL in 40 μL of EMEM, 10% FCS, 1% glutamine and grown for 24 h. Following addition of compound the cells are incubated for 60 min. A final concentration of 3 μM 4NQO (prepared in 100% DMSO) is then added using the Labcyte Echo, and the cells are incubated for a further 60 min. The cells are fixed by adding 40 μL of 3.7% v/v formaldehyde solution for 20 min. After removal of fix, cells are washed with PBS and permeabilized in 40 μL of PBS containing 0.1% Triton X-100. The cells are then washed, and 15 μL primary antibody solution (pChk1 Ser345) is added. The plates are incubated at 4°C overnight. The primary antibody is then washed off, and 20 μL of secondary antibody solution and 1 μM Hoechst 33258 added for 90 min at room temperature. The plate

• 參考文獻(xiàn)：
  1. Foote KM, et al. Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity. J Med Chem, 2013, 56(5), 2125-2138.

• 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	2.424 ml	12.121 ml	24.242 ml
  5 mM	0.485 ml	2.424 ml	4.848 ml
  10 mM	0.242 ml	1.212 ml	2.424 ml
  50 mM	0.048 ml	0.242 ml	0.485 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 *