Mubritinib (Tak-165) (CAS: 366017-09-6)

Mubritinib (Tak-165)  is a potent Neu (HER2) and Cdc2 p34 inhibitor with IC50 of 6 nM and 0.2μM, respectively. TAK 165 also inhibits p33cdk2 and 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. 

Basic Information

Mubritinib (TAK-165) is a protein kinase inhibitor which was under development by Takeda for the treatment of cancer. It completed phase Iclinical trials but appears to have been discontinued, as no new information on the drug has surfaced since December 2008.