FPA-124是Akt結(jié)合PH和激酶結(jié)構(gòu)域的細胞滲透性抑制劑(IC 50 = 100 nM)。它抑制Colo 357 BxPC 3 BT 20和PC 3癌細胞系中的細胞增殖,IC 50值范圍為7-55 nM。FPA-124抑制小鼠腫瘤生長,毒性可忽略不計。參考文獻由Bioz提供支持參見Bioz的更多詳細信息1)V. Barve等人,“Synthesis Molecular Characterization and Biological Activity of Novel SyntheticDerivatives of Chromen-4-one in Human Cancer Cells”J. Med. Chem. 2006 49 3800- 3808。 G. Straface等人(2009年)。“吡格列酮通過Akt依賴性VEGF介導(dǎo)的機制增強糖尿病小鼠缺血后肢的側(cè)支血流量,而不管PPARgamma刺激如何。“Bavasc Diabetol 8:49.3)Brito P. M. R. L. Devillard等人(2009)。“白藜蘆醇抑制平滑肌細胞中氧化LDL誘發(fā)的mTOR有絲分裂信號。“Atherosclero205(1):126。
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FPA-124 is a cell-permeable inhibitor of Akt (IC50 = 100 nM) binding to the PH and kinase domains. It inhibits cell proliferation in Colo357 BxPC3 BT20 and PC3 cancer cell lines with IC50 values ranging from 7-55 nM. FPA-124 inhibited tumor growth in mice with negligible toxicity.References Powered by Bioz See more details on Bioz1) V. Barve et al. "Synthesis Molecular Characterization and Biological Activity of Novel SyntheticDerivatives of Chromen-4-one in Human Cancer Cells" J. Med. Chem. 2006 49 3800-3808.2) Biscetti F. G. Straface et al. (2009). "Pioglitazone enhances collateral blood flow in ischemic hindlimb of diabetic mice through an Akt-dependent VEGF-mediated mechanism regardless of PPARgamma stimulation." Cardiovasc Diabetol 8: 49.3) Brito P. M. R. l. Devillard et al. (2009). "Resveratrol inhibits the mTOR mitogenic signaling evoked by oxidized LDL in smooth muscle cells." Atherosclerosis 205(1): 126.