883561-04-4

CA-224 is potent CDK4 inhibitor, is also a nonplanar analogue of fascaplysin that specifically inhibits Cdk4-cyclin D1 in vitro. CA-224 blocks the growth of cancer cells at G0/ G1 phase of the cell cycle. CA-224 also blocks the cell cycle at G2/M phase, which is explained by the fact that it inhibits tubulin polymerization. Additionally, CA-224 acts as an enhancer of depolymerization for taxol-stabilized tubulin. CA-224 selectively induces apoptosis of SV40 large Tantigen. transformed cells and significantly reduces colony formation efficiency, in a dose-dependent manner, of lung cancer cells. The promising efficacy of CA-224 in human xenograft models as well as its excellent therapeutic window indicates its potential for clinical development.

CA224 (Compound 1) 是一种选择性的、具有口服活性的 Cdk4–cyclin D1 抑制剂， IC50 值为 6.2 µM。CA224 诱导细胞凋亡 (apoptosis)，具有抗肿瘤活性。