Tirbanibulin dihydrochloride

Description: Tirbanibulin dihydrochloride (also known as KXO1 dihydrochloride and KX2-391 dihydrochloride) is novel, potent and the first clinical peptidomimetic Src inhibitor that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. KX2-391 is an orally bioavailable small molecule with potential antineoplastic activity. Unlike other Src kinase inhibitors which bind to the ATP-binding site, Src kinase inhibitor KX2-391 specifically binds to the peptide substrate binding site of Src kinase; inhibition of kinase activity may result in the inhibition of primary tumor growth and the suppression of metastasis. Src tyrosine kinases are upregulated in many tumor cells and play important roles in tumor cell proliferation and metastasis.

References: Dig Dis Sci. 2009 Jul; 54(7):1465-74; Eur J Med Chem. 2011 Oct; 46(10):4853-8.

Related CAS#: 897016-82-9 (Tirbanibulin free base); 1080645-95-9 (Tirbanibulin Mesylate)