Tubulin-IN-57 is a tubulin inhibitor and a potent antiproliferative agent that suppresses colony formation, migration, and invasion of ovarian cancer cells. It disrupts tubulin polymerization, inducing G2/M phase arrest and apoptosis (apoptosis) in SKOV3 cells. In SKOV3 xenograft tumor models, Tubulin-IN-57 demonstrates significant antitumor activity without noticeable toxicity. It is applicable for ovarian cancer research.

Tubulin-IN-57 (Compound Y60s) exhibits potent antiproliferative activity with an IC50 of 0.025 μM for SKOV3 cells and 0.026 μM for A549 cells. At concentrations of 25-200 nM over 6 days, it hinders colony formation and proliferation of SKOV3 and A549 cells. Tubulin-IN-57 also suppresses cell migration of these cell lines within a 24-hour period using the same concentration range. Additionally, it induces apoptosis and alters the expression of apoptosis-related proteins in SKOV3 and A549 cells after 48 hours when used at 25-200 nM concentrations. The compound causes G2/M phase cell cycle arrest in both cell lines after a 24-hour exposure at 25, 50, 100, or 200 nM. Tubulin-IN-57 inhibits tubulin polymerization in a dose-dependent manner, entirely preventing polymerization at 20 μM. Furthermore, a dose of 20 nM causes significant destruction and disruption of microtubules in SKOV3 cells.

Tubulin-IN-57 (2 mg/kg, 4 mg/kg, intravenous injection, every 2 days for a total of 12 times) inhibits tumor growth by suppressing cell proliferation, and does not exhibit significant pathological changes in mice. This suggests minimal toxicity at the tested dosages and regimen.