We found that inhibition PFKFB3 by PFK15, which is about 100-fold more potent than 3PO toward PFKFB324, cooperates with cisplatin to promote cancer cell apoptosis and significantly potentiates the inhibitory effect of cisplatin on tumor growth, providing further evidence that PFKFB3 inhibitor, such as PFK15, merits to be exploited in cancer treatment. This evidence concerns the gene PFKFB3 and neoplasm.