compound introduction
SU9516是在肿瘤细胞中表现出抗增殖和促凋亡特性的3-取代的吲哚满酮化合物。SU9516显示出作为CDK的选择性强效ATP竞争性抑制剂的活性。它还对PKC，p38，PDGFRβ或EGFR的活性无明显影响（IC | 50 |> 10μM）。SU9516通过与Cdk2结合并阻止pRb的磷酸化及其从E2F的解离，对生长因子刺激的结肠癌细胞的增殖具有抑制作用。SU9516是Cdc2，Cdk2和Cdk4的抑制剂。 SU9516 is a 3-substituted indolinone compound displaying anti-proliferative and proapoptotic properties in tumor cells. SU9516 displays activity as a selectively potent ATP-competitive inhibitor of CDKs. It also shows no significant effect (IC|50|>10 μM) on the activities of PKC, p38, PDGFRβ, or EGFR. SU9516 has an Inhibitory effect on proliferation of growth-factor stimulated colon carcinoma cells by binding to Cdk2 and preventing the phosphorylation of pRb and its dissociation from E2F. SU9516 is an inhibitor of Cdc2, Cdk2 and Cdk4.
