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Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.

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Burchat A., Borhani D.W., Calderwood D.J., Hirst G.C., Li B., Stachlewitz R.F.

We describe the identification, SAR, and pharmacology of the src-family selective lck inhibitor A-770041 that prolongs the survival of major histocompatibility mismatched allografts in models of solid organ transplant rejection for greater than 65 days.

Bioorg. Med. Chem. Lett. 16:118-122(2006) [PubMed] [Europe PMC]