SB-267268 inhibits human and mouse αvβ3 (IC50s: 0.68 and 0.29 nM, respectively). SB-267268 is a selective and nonpeptidic alpha(v)beta3 and alpha(v)beta5 integrins antagonist (Kis: 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively).

SB-267268 inhibits the attachment of bothαvβ3-transfected HEK293 cells to microtiter plate wells precoated with arginine-glycine-aspartic acid (RGD)-containing matrix proteins (IC50: 12 nM). SB-267268 also inhibits vitronectin-mediated human and rat aortic smooth-muscle-cell (SMC) migration (IC50: approximately 12.3 nM and 3.6 nM, respectively) [1].

SB-267268 (60 mg/kg; bi-daily, i.p.) decreases blood vessel profiles (BVPs) in the inner retina by 50%. VEGF and VEGFR-2 gene expression in the inner nuclear layer (INL) and the ganglion cell layer (GCL) is reduced in ROP mice treated with SB-267268 [1].