Tubulin-IN-54 is a tubulin inhibitor exhibiting antiproliferative effects against various cancer cell lines. It disrupts microtubule assembly, leading to the breakdown of the microtubule network, inducing G2/M phase cell cycle arrest, and promoting apoptosis in cancer cells. Additionally, Tubulin-IN-54 demonstrates significant antitumor efficacy in mice with PC-3/TxR xenografts. It is applicable in studies of paclitaxel-resistant cancers, such as prostate cancer and melanoma.

Tubulin-IN-54 (Compound 11b) exhibits potent antiproliferative activity against human melanoma cells A375 (IC 50 = 0.6 nM) and M14 (IC 50 = 0.6 nM), as well as human prostate cancer cells PC-3 (IC 50 = 1.3 nM) over 72 hours. Additionally, Tubulin-IN-54 (2-5 nM, 24 h) inhibits microtubule polymerization and disrupts microtubule network structures in PC-3/TxR cells. It also strongly inhibits colony formation and migration in PC-3/TxR cells at 0.5-5 nM for 24 hours. Furthermore, Tubulin-IN-54 (1-5 nM, 24 h) induces G2/M phase cell cycle arrest and apoptosis in PC-3/TxR cells.

Tubulin-IN-54 (Compound 11b) (15 mg/kg, intraperitoneal injection, 5 times a week for 2 weeks) demonstrated significant antitumor activity in NSG male mice with PC-3/TxR prostate cancer xenografts.