LY2510924 acetate(1088715-84-7 free base) 是一种有效的选择性 CXCR4 拮抗剂。它可防止 SDF-1 与 CXCR4 结合，IC50 为 0.079 nM。

Ly2510924 acetate is an potent and selective CXCR4 antagonist. It prevents the binding of SDF-1 to CXCR4 with an IC50 of 0.079 nM.

In human lymphoma U937 cells expressing endogenous CXCR4, LY2510924 acetate inhibited SDF-1-induced cell migration with IC50 value of 0.26 nmol/L and inhibited SDF-1/CXCR4-mediated intracellular signaling. LY2510924 acetate exhibited a concentration-dependent inhibition of SDF-1-stimulated phospho-ERK and phospho-Akt in tumor cells.

LY2510924 acetate showed dose-dependent inhibition of tumor growth in human xenograft models developed with non-Hodgkin lymphoma, renal cell carcinoma, lung, and colon cancer cells that express functional CXCR4. In MDA-MB-231, a breast cancer metastatic model, LY2510924 acetate inhibited tumor metastasis by blocking migration/homing process of tumor cells to the lung and by inhibiting cell proliferation after tumor cell homing.

T15805L

C64H91N13O13

1250.49

DMSO:60 mg/ml (47.98 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years