CXCR4 Antagonist III

A cell-permeable quinazoline compound that acts as a potent and reversible CXCR4 antagonist (IC₅₀ = 36.2 nM for SDF-1/CXCL12 binding to hCXCR4-transfected HEK293 membrane) with selectivity over closely related human chemokine receptors CXCR2, CCR2, CCR4 and CCR5 (IC₅₀ >10 µM). Shown to inhibit CXCL12-induced Ca²⁺-mobilization and cell migration in hCXCR4-HEK293 cells (IC₅₀ = 100.1 and 41 nM, respectively), and rapidly mobilize CXCR4⁺, CD34⁺ and CD133⁺ stem cells from bone marrow in C57BL/6 male mice (6 mg/kg, s.c).

Cell permeable: yes

Reversible: yes

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (20°C). Stock solutions are stable for up to 6 months at -20°C.

Wu, C.H., et al. 2012. Chem. Med. Chem.7, In press.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany