Biological Activity
u-104 is a novel ureido-sulfonamide inhibitor of carbonic anhydrase ix (caix). tumor volume measurements show important inhibition of primary tumor growth in the mice treated with the u-104 compound compared with vehicle controls. it also has ability to inhibit metastasis formation in the 4t1 experimental metastasis model.yuanmei lou, paul c. mcdonald, arusha oloumi, stephen chia, christina ostlund, ardalan ahmadi, alastair kyle, ulrich auf dem keller, samuel leung, david huntsman, blaise clarke, brent w. sutherland, dawn waterhouse, marcel bally, calvin roskelley, christopher m. overall, andrew minchinton, fabio pacchiano, fabrizio carta, andrea scozzafava, nadia touisni, jean-yves winum, claudiu t. supuran, shoukat dedhar. targeting tumor hypoxia: suppression of breast tumor growth and metastasis by novel carbonic anhydrase ix inhibitors. cancer research may 1, 2011 71; 3364
Biochem/physiol Actions
U-104 is an inhibitor of CA IX that binds only to CA IX under hypoxic conditions in vivo. The binding results in significant inhibition of tumor growth and metastasis formation in both spontaneous and experimental models of metastasis. U-104 reduces the medium acidity by inhibiting the catalytic activity of the CA IX. It binds specifically only to hypoxic cells expressing CA IX.
