Potent Ack1 (TNK2) inhibitor (IC50
= 22 nM). Exhibits selectivity for Ack1 over ABL1, BTK, Lck and LYN; exhibits no inhibition of 25 other kinases. Suppresses phosphorylation of Tyr267 of the androgen receptor in prostate cancer cells. Also suppresses growth of radioresistant castration-resistant prostate cancer in xenograft tumors in mice.
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All Tocris products are intended for laboratory research use only.
Ack1-mediated androgen receptor phosphorylation modulates radiation resistance in castration-resistant prostate cancer.
Mahajan K, Coppola D, Rawal B et al.
J Biol Chem
Effect of Ack1 tyrosine kinase inhibitor on ligand-independent androgen receptor activity.
Mahajan et al.