ENMD-2076

一种多激酶抑制剂；抑制FLT3、RET和Aurora A激酶（IC50分别为1.86、10.4和14nM）；还抑制参与血管生成的其他激酶（IC50<50nM）；通过口服灌胃给药（100mg/kg）降低肿瘤血管通透性和灌注，抑制人三阴性乳腺癌（TNBC）和结直肠癌小鼠异种移植模型中的肿瘤生长。A multi-kinase inhibitor; inhibits FLT3, RET, and Aurora A kinase (IC50s = 1.86, 10.4, and 14 nM, respectively); inhibits additional kinases involved in angiogenesis (IC50s = 50s = via oral gavage); decreases tumor vascular permeability and perfusion and inhibits tumor growth in human TNBC and colorectal cancer mouse xenograft models of (100 mg/kg via oral gavage).