TAK 165 is a potent Neu (HER2) and Cdc2 p34 inhibitor with IC50 of 6 nM and 0.2μM, respectively. TAK 165 also inhibits Cdk2 (p33cdk2) and Cdk5 (p33cdk5). TAK 165 displays > 4000-fold selectivity over EGFR, FGFR, PDGFR, JAK1 and Src. TAK 165 exhibits potent antiproliferative effects in Neu-overexpressing cancer cell lines (IC50 = 5 nM in BT474 breast cancer cells) and significantly inhibits bladder, breast and prostate cancer xenograft growth.
1. Nagasawa, J., et al. 2006. Int. J. Urol. 13: 587-592 .PMID: 16771730