XMU-MP-2

XMU-MP-2 is a selective BRK/PTK6 inhibitor with an IC₅₀ of 5.4 nM. XMU-MP-2 inhibits the proliferation of BRK-positive breast cancer cells and induces apoptosis. XMU-MP-2 is applicable to breast cancer-related research^[1]. In Vitro:XMU-MP-2 (10-5000 nM; 4-48 h) inhibits the proliferation of BRK-transformed Ba/F3 cells with an IC₅₀ of 29.7 nM, blocks BRK-mediated signaling pathways, and induces dose-dependent apoptosis^[1].
XMU-MP-2 (50-5000 nM; 4-48 h) shows significantly reduced potency against BRK^T264M-transformed Ba/F3 cells (IC₅₀ = 340.4 nM)^[1].
XMU-MP-2 (50-5000 nM; 4-48 h) potently inhibits the proliferation of BRK^Y447F-transformed Ba/F3 cells with an IC₅₀ of 91.0 nM, blocks BRK-mediated signaling pathways and induces apoptosis^[1].
XMU-MP-2 (50-10000 nM; 48 h) selectively inhibits the proliferation of BRK-positive breast cancer cell lines (BT-474, BT-20, MCF7, T-47D)^[1].
XMU-MP-2 (0-16 μM; 0-3 days) exhibits strong synergistic antiproliferative effects with the HER2 inhibitor CP-724714 (HY-14674) in BT-474 cells, and with 4-Hydroxytamoxifen (HY-16950) in MCF7 cells^[1]. In Vivo:XMU-MP-2 (10-40 mg/kg; intravenous injection; once daily; 14 days) significantly inhibits tumor growth and induces tumor cell apoptosis in BRK-positive breast cancer xenograft models of female BALB/c nude mice^[1].