AZM475271

c-Src激酶抑制剂(IC50=0.01µM)；抑制c-Src激酶、Lck、c-Yes和VEGFR2的磷酸化(IC50s分别为0.01、0.03、0.08和0.7µM)；抑制NIH3T3成纤维细胞以及PC3、DU145和A549癌细胞的增殖(IC50s分别为0.5、32、16和17µM)；在L3.6pl胰腺癌小鼠异种移植模型中，以50mg/kg/天的剂量降低肿瘤细胞增殖和微血管密度并增加细胞凋亡；与吉西他滨联合使用可抑制同一模型中的肿瘤生长和转移。An inhibitor of c-Src kinase (IC50 = 0.01 µM); inhibits phosphorylation of c-Src kinase, Lck, and c-Yes, and VEGFR2 (IC50s = 0.01, 0.03, 0.08, and 0.7 µM, respectively); inhibits proliferation of NIH3T3 fibroblasts, as well as PC3, DU145, and A549 cancer cells (IC50s = 0.5, 32, 16, and 17 µM, respectively); reduces tumor cell proliferation and microvessel density and increases apoptosis in an L3.6pl pancreatic cancer mouse xenograft model at 50 mg/kg per day; inhibits tumor growth and metastasis in the same model in combination with gemcitabine.分子式C23H27ClN4O3分子量442.9ClC1=CC=C(C=C1NC2=C3C=C(OC)C(OCC4CCN(CC4)C)=CC3=NC=N2)OC