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