Tirbanibulin CAS# 897016-82-9 5-[4-[2-(4-吗啉基)乙氧基]苯基]-N-(苯基甲基)-2-吡啶乙酰胺

Tirbanibulin (KX2-391 or KXB-964) is a synthetic, dual-action inhibitor of Src kinase signaling and tubulin polymerization. In preclinical biochemical assays, it inhibited Src kinase activity with an IC50 of ~9 nM and blocked tubulin polymerization with an IC50 of ~120 nM, leading to mitotic arrest and apoptosis in proliferating cells. In cancer cell lines, tirbanibulin suppressed proliferation and induced G2/M arrest at low nanomolar concentrations. In xenograft mouse models, topical or systemic administration produced significant tumor growth inhibition without notable systemic toxicity. These findings supported its development as a topical antiproliferative agent for actinic keratosis and other skin lesions.