3-(4-吗啉代噻吩并[3 2-d]嘧啶-2-基)苯酚是PI 3-激酶的β ±-亚型的选择性抑制剂(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))。它显示出对蛋白激酶如PKA、KDR、PKCa和E/CDK 2的1000倍选择性(IC 50 = 91 3.4 466 288 μ M)。它在580 nM时抑制A375黑色素瘤细胞的增殖。也被称为PI 3-K抑制剂2 PIK 2。参考资料由Bioz提供技术支持。Hayakawa等人,“4-morpholino-2-phenyl quinazolines and related derivatives as novel PI3 kinase p110a inhibitors”Bioorg. 2006 14 6847-6858。
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3-(4-Morpholinothieno[3 2-d]pyrimidin-2-yl)phenol is a selective inhibitor for the α-isoform of PI 3-Kinase (IC50: PI 3-Kα = 2 nM PI 3-Kβ = 16 nM PI3-Kγ = 660 nM PI3KC2β = 220 nM)). It showed >1000-fold selectivity vs. protein kinases such as PKA KDR PKCa and E/CDK2 (IC50 = 91 3.4 466 288 μM). 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.