WZ811

WZ811 is an orally active, highly potent competitive antagonist of CXCR4. WZ811 efficiently inhibits CXCR4/SDF-1 (or CXCL12)-mediated modulation of cAMP levels (EC₅₀=1.2 nM) and SDF-1 induced Matrigel invasion in cells (EC₅₀=5.2 nM)^[1]. IC50 & Target:CXCR4^[1] In Vitro: WZ811 (Compound 32) is a potent CXCR4 antagonist, effectively inhibits TN14003 binding to CXCR4, with an EC₅₀ of 0.3 nM^[1].
WZ811 blocks SDF-1 mediated modulation cAMP levels in U87 glioma cells (EC₅₀=1.2 nM) and Matirgel infiltration of MDA-MB-231 cells (EC₅₀=5.2 nM)^[1].
WZ811 (1-40 μM) inhibits TF-1 and UT-7 cells proliferation in a dose dependent manner both after treatment for 24 h and 48 h. Moreover, WZ811 (5 μM) induces cell apoptosis and enhances the sensitivity of cells to docetaxel. In addition, WZ811 inhibits aggressiveness markers and induces apoptosis in chronic lymphocytic leukemia cells^[2]. In Vivo: WZ811 (40 mg/kg, p.o.) blocks the lymphocytic leukemia cells growth on mouse xenograft models, and inhibits CXCR4/PI3K/AKT signaling pathway in mouse xenograft model of lymphocytic leukemia^[2].