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Chemical Compound Review:

AC1LAPYA 3-[2-[[3- (diaminomethylideneamino) phenyl]c...

Synonyms: SureCN244261, SC-68448, SC68448

Carron, C.P. et al.

Carron, Meyer, Pegg, Engleman, Nickols, Settle, Westlin, Ruminski, Nickols,

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Disease relevance of SC-68448

A xenogeneic severe combined immune deficiency mouse/rat Leydig cell tumor model was developed for testing SC-68448 as an inhibitor of tumor growth in vivo [1].
SC-68448 inhibited the growth of the tumors in mice by up to 80% and completely blocked the development of hypercalcemia [1].
In accord with these results, SC-68448 inhibited angiogenesis in vivo in a basic fibroblast growth factor-induced rat corneal neovascularization model [1].

High impact information on SC-68448

One of these compounds, beta-[[2-2-[[[3-[(aminoiminomethyl)amino]-phenyl]carbonyl]amino]ac etyl]amino]-3,5-dichlorobenzenepropanoic acid (SC-68448), inhibited vitronectin binding to both alpha(v)beta3 and the closely related platelet receptor, alpha(IIb)beta3, in a dose-responsive manner [1].
In cell-based studies, SC-68448 inhibited alpha(v)beta3-mediated endothelial cell proliferation in a dose-dependent manner but did not inhibit tumor cell proliferation, suggesting that effects on endothelial cell proliferation were not due to SC-68448-induced cytotoxicity [1].

Biological context of SC-68448

SC-68448 inhibited vitronectin binding to alpha(v)beta3 (IC50, 1 nM) and fibrinogen binding to the platelet receptor alpha(IIb)beta3 (IC50, >100 nM), demonstrating that SC-68448 was 100-fold more potent as an inhibitor of alpha(v)beta3 versus alpha(IIb)beta3 [1].

References

A peptidomimetic antagonist of the integrin alpha(v)beta3 inhibits Leydig cell tumor growth and the development of hypercalcemia of malignancy. Carron, C.P., Meyer, D.M., Pegg, J.A., Engleman, V.W., Nickols, M.A., Settle, S.L., Westlin, W.F., Ruminski, P.G., Nickols, G.A. Cancer Res. (1998) [Pubmed]

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