Compound class:
Synthetic organic
Comment: KC-180-2 is a dual action tubulin polymerisation inhibitor and Src kinase inhibitor that was developed as a refined derivative of the anti-cancer agent tirbanibulin (KX2-391) [1]. Destabilisation of tubulin polymers is the primary mechanism that underlies KC-180-2's effects on cell cycle arrest in cancer cells. KC-180-2 occupies the same non-ATP substrate binding pocket within Src as KX2-391.
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Bioactivity Comments |
KC-180-2 exhibits favourable anti-proliferative activity against human cancer cell lines in vitro, with highest efficacy against NCI-H446 (human lung adenocarcinoma; SCLC) cells (IC50 4.8 nM). It is active in vivo, inhibiting tumour growth in an NCI-H446 xenograft model. |