WJD008 is a potent dual phosphatidylinositol 3-kinase ( PI3K )/mammalian target of rapamycin ( mTOR ) inhibitor with antiproliferative and anticlonogenic activity in tumor cells and transformed cells with PIK3CA mutant. WJD008 inhibits kinase activity of PI3K α and mTOR and abrogates insulin-like growth factor-I-activated PI3K-Akt-mTOR signaling cascade. WJD008 is promising for research of cancers.