1464842-09-8
1464842-09-8 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
沸點755.6±60.0 °C(Predicted)
密度1.496±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)11.51±0.20(Predicted)
形態(tài)Solid
顏色Off-white to light yellow
應(yīng)用領(lǐng)域
用途一
M8891 is a potent and orally active methionine aminopeptidase 2 inhibitor with potential antiangiogenic and antineoplastic activities. Upon administration, MetAP2 inhibitor M8891 inhibits MetAP2 aminopeptidase activity and impairs protein synthesis, which may lead to a decrease in endothelial cell proliferation. Decreased proliferation of endothelial cells results in reductions of both angiogenesis and the growth and spread of solid tumors that are dependent on new blood vessel formation. MetAP2, a metallopeptidase, is involved in promoting protein synthesis and endothelial cell proliferation.常見問題列表
概述
M8891 是一種具有口服活性，可逆的且能透過血腦屏障的甲硫氨酸氨基肽酶 2 (MetAP-2) 抑制劑，IC50 為 54 nM，Ki 為 4.33 nM。M8891 不抑制 MetAP-1 (IC 50>10 μM)。M8891 抑制原代內(nèi)皮細(xì)胞以及腫瘤細(xì)胞的生長，具有抗血管生成和抗腫瘤活性。