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SM-1, N'-(3-allyl-2-hydroxy-benzylidene)-2-(4-benzyl-1,4-homopiperazi-ne-1-yl) acetohydrazide fumarate salt, is a newly synthesized small molecule compound displaying a strong antitumor activity.SM-1 can specifically activate the procaspase-3 and transform it into caspase-3, thus killing the cancer cell.SM-1 was mainly excreted through metabolism after intragastric administration.