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產品描述： VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM. |
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靶點：
ATR：13 nM (Ki)；ATM：16 μM (Ki)；DNA-PK：2.2 μM (Ki)；PI3Kγ：3.9 μM (Ki);ATM/ATR |
參考文獻：
1. Reaper PM, et al. Selective killing of ATM- or p53-deficient cancer cells through inhibition of ATR. Nat Chem Biol. 2011 Apr 13;7(7):428-30. 2. Charrier JD, et al. Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents. J Med Chem. 2011 Apr 14;54(7):2320-30. 3. Prevo R, et al. The novel ATR inhibitor VE-821 increases sensitivity of pancreatic cancer cells to radiation and chemotherapy. Cancer Biol Ther. 2012 Sep;13(11):1072-81. 4. Muralidharan SV, et al. BET bromodomain inhibitors synergize with ATR inhibitors to induce DNA damage, apoptosis, senescence-associated secretory pathway and ER stress in Myc-induced lymphoma cells. Oncogene. 2016 Sep 8;35(36):4689-97. |
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溶解性：
DMSO : 50 mg/mL (135.72 mM; Need ultrasonic) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) |
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保存條件：
-20℃ |
配置溶液濃度參考：
|
1mg |
5mg |
10mg |
| 1 mM |
2.714 ml |
13.572 ml |
27.144 ml |
| 5 mM |
0.543 ml |
2.714 ml |
5.429 ml |
| 10 mM |
0.271 ml |
1.357 ml |
2.714 ml |
| 50 mM |
0.054 ml |
0.271 ml |
0.543 ml |
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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京