KX2-391

KX2-391 is a synthetic, orally bioavailable small molecule and non-ATP competitive Src tyrosine kinase signaling inhibitor with an IC50 of average 72 nM. KX2-391 has potential antineoplastic activity. Src kinase inhibitor KX2-391 specifically binds to the peptide substrate binding site of Src kinase. In addition, KX2-391 also inhibits microtubule polymerization. Preclinical studies have suggested that KX2-391 is able to prevent the proliferation and metastasis of prostate cancer cell lines in mouse xenografts. KX2-391 phase I clinical trials have been completed.