XMU-MP-2 (XMU-MP2) is a novel, potent and selective inhibitor of BRK/PTK6 (breast tumor kinase) with anti-cancer activity. It inhibits BRK with an IC50 of 3.2 nM, and inhibits the autophosphorylation of BRK Y342 dose-dependently (maximum inhibition at 500 nM). Also abolishes phosphorylation levels of STAT3 Y705 and STAT5 Y694. In addition,it blocks proliferation and survival of BRK-transformed Ba/F3 cells with IC50 of 29.7 nM; Moreover, the combination of XMU-MP-2 with HER2 inhibitor or ER blockade suppressed breast cancer cell proliferation in vitro and in vivo. Approximately 80% of breast cancers overexpress the kinase breast tumor kinase (BRK)/protein tyrosine kinase 6, which has various oncogenic roles in breast cancer cell proliferation, survival, and migration.

纯度：≥98%

CAS：2031152-10-8