1257994-15-2
1257994-15-2 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
沸點(diǎn)827.4±75.0 °C(Predicted)
密度1.299±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)8.20±0.42(Predicted)
應(yīng)用領(lǐng)域
用途一
OXA-11 is a potent, novel small-molecule amino pyrimidine inhibitor (1.2 pM biochemical IC(50)) of focal adhesion kinase (FAK). OXA-11 inhibited FAK phosphorylation at phospho-tyrosine 397 with a mechanistic IC(50) of 1 nM in TOV21G tumor cells, which translated into functional suppression of proliferation in 3-dimensional culture with an EC(50) of 9 nM. Studies of OXA-11 activity in TOV21G tumor-cell xenografts in mice revealed a pharmacodynamic EC(50) of 1.8 nM, indicative of mechanistic inhibition of pFAK [Y397] in these tumors. OXA-11 slows tumor growth, potentiates the anti-tumor actions of cisplatin and--when combined with VEGFR-2 blockade--reduces metastasis of pancreatic neuroendocrine tumors in RIP-Tag2 mice.