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AZ20 99%

(R)-4-(2-(1H-indol-4-yl)-6-(1-(methylsulfonyl)cyclopropyl)pyrimidin-4-yl)-3-methylmorpholine

源葉(MedMol)
S81255
1233339-22-4
C21H24N4O3S
412.51
品牌 貨號 產品規格 價格(RMB) 庫存（上海） 北京 武漢 南京 購買數量
源葉(MedMol) S81255-5mg 99% ￥400.00元 4 - - -
源葉(MedMol) S81255-10mg 99% ￥700.00元 5 - - -
源葉(MedMol) S81255-25mg 99% ￥1400.00元 5 - - -
源葉(MedMol) S81255-100mg 99% ￥3800.00元 2 - - -
產品介紹 參考文獻 質檢證書(COA) 摩爾濃度計算器 相關產品

產品介紹

AZ20 is an effective and specific inhibitor of ATR kinase (IC50: 5 nM, in a cell-free assay), 8-fold selectivity over mTOR
產品描述： 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： mTOR;ATM/ATR;ATM/ATR;?mTOR
體外研究：
AZ20（10 μM）可使CYP3A4介導的咪達唑侖代謝的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. ）可使腫瘤生長受到顯著抑制,這與異種移植組織中γH2AX核染色的持續廣泛升高有關
體內研究：
在體外,AZ20濃度依賴性地降低pChk1 Ser345/317/296水平。延長AZ20的處理時間可增加γH2AX核染色,這是因為存在復制壓力,且與S期阻滯和組蛋白H3的磷酸化水平增加有關。AZ20對體外生長抑制和細胞死亡的誘導作用是完全不同于其它細胞毒性藥物的。AZ2與ATM 抑制劑KU-60019聯用會增加細胞毒性
細胞實驗： 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：
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
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參考文獻

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摩爾濃度計算器

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