3-（4-嗎啉代噻吩并[3 2-d]嘧啶-2-基）苯酚是PI 3-激酶的β ±-亞型的選擇性抑制劑（IC 50：PI 3-KC ± = 2 nM PI 3-KC 2 = 16 nM PI 3-KC 3 = 660 nM PI 3 KC 2 = 220 nM））。它顯示出對蛋白激酶如PKA、KDR、PKCa和E/CDK 2的1000倍選擇性（IC 50 = 91 3.4 466 288 μ M）。它在580 nM時抑制A375黑色素瘤細胞的增殖。也被稱為PI 3-K抑制劑2 PIK 2。參考資料由Bioz提供技術支持。Hayakawa等人，“4-morpholino-2-phenyl quinazolines and related derivatives as novel PI3 kinase p110a inhibitors”Bioorg. 2006 14 6847-6858。
產品描述
3-(4-Morpholinothieno[3 2-d]pyrimidin-2-yl)phenol is a selective inhibitor for the ?±-isoform of PI 3-Kinase (IC50: PI 3-K?± = 2 nM PI 3-K?2 = 16 nM PI3-K?3 = 660 nM PI3KC2?2 = 220 nM)). It showed >1000-fold selectivity vs. protein kinases such as PKA KDR PKCa and E/CDK2 (IC50 = 91 3.4 466 288 ??M). It inhibited proliferation of A375 melanoma cells at 580 nM. Also known as PI3-K Inhibitor 2 PIK2.References Powered by Bioz See more details on Bioz1) M. Hayakawa et al. "Synthesis and biological evaluation of 4-morpholino-2-phenyl quinazolines and related derivatives as novel PI3 kinase p110a inhibitors" Bioorg. Med. Chem. 2006 14 6847-6858.
