品牌	貨號	產(chǎn)品規(guī)格	價格(RMB)	庫存（上海）	北京	武漢	南京
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(chǎn)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(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： 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AZ20的處理時間可增加γH2AX核染色,這是因為存在復(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對體外生長抑制和細(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)用會增加細(xì)胞毒性

細(xì)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(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：

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參考文獻(xiàn)

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AZ20 99%

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