S80135
具體成交價以合同協議為準
- 公司名稱 上海源葉生物科技有限公司
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- 產地
- 廠商性質 生產廠家
- 更新時間 2024/7/4 7:43:06
- 訪問次數 243
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- 產品描述： A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.
- 靶點： p110α:32 nM (IC50);p110α E545K:30 nM (IC50);p110α H1047R:43 nM (IC50);p110γ:3480 nM (IC50);PI3K-C2β:462 nM (IC50);PI4Kβ:236 nM (IC50)
- 體內研究： The optimal dosing strategy for xenograft studies is determined by investigating the drug pharmacokinetics after a dose of 10 mg/kg of body weight by intraperitoneal injection in CD-1 mice. Despite a short half-life of only 0.42 h, the large Cmax (8247 nM) of A66 S that is reached 30 min after dosing ensured that the AUC0-inf (area under the curve from zero time to infinity) (6809 nM?h) is similar to that of BEZ-235 (7333 nM?h), which has a longer half-life of 2.73 h. Furthermore, the A66 on SK-OV-3 tumour tissue is tested using a single dose of 100 mg/kg of body weight to determine whether a long-lasting effect of the drug could be achieved on target tissues. These studies show that A66 causes a profound reduction in the phosphorylation of Akt/PKB and p70 S6 kinase, but not of ERK (extracellular-signal-regulated kinase), at both 1 and 6 h after dosing. Levels of A66 in plasma are determined to be 21.1±1.2 μM and 9.1±1.1 μM at 1 and 6 h after drug injection, whereas levels of A66 in the tumor are 22.7±2.1 μM and 16.0±1.3 μM at the same time points
- 參考文獻：
1. Jamieson S, et al. A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem J, 2011, 438(1), 53-62. 2. Sun M, et al. Cancer-derived mutations in the regulatory subunit p85alpha of phosphoinositide 3-kinase function through the catalytic subunit p110alpha. Proc Natl Acad Sci U S A, 2010, 107(35), 15547-15552.
- 溶解度： DMSO : 50 mg/mL (127.06 mM; Need ultrasonic)
- 保存條件： -20℃
- 配置溶液濃度參考：
1mg 5mg 10mg 1 mM 2.541 ml 12.706 ml 25.411 ml 5 mM 0.508 ml 2.541 ml 5.082 ml 10 mM 0.254 ml 1.271 ml 2.541 ml 50 mM 0.051 ml 0.254 ml 0.508 ml
- 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性，僅供客戶參考交流研究之用。
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