Tubulin polymerization-IN-14 (Compound 20a) is a tubulin polymerization inhibitor (IC50 = 3.15 μM) that demonstrates strong anti-vascular and anticancer activities, including inducing cancer cell apoptosis [1].

Tubulin polymerization-IN-14 (Compound 20a) targets the colchicine binding site on tubulin to inhibit cancer cell growth at concentrations of 0-1 μM over 72 hours. At lower concentrations (5-20 nM) over 48 hours, it halts the cell cycle in the G2/M phase and triggers apoptosis in K562 cells dose-dependently, causing mitochondrial membrane potential collapse and dysfunction. Over 24 hours at similar concentrations, it reduces wound closure and capillary-like structure formation in HUVECs, suggesting potential anti-angiogenic properties. It demonstrates an anti-proliferative effect with an IC50 of 0.01 ± 0.001 μM against K562 cells and exhibits cytotoxic activity against HepG2, HCT-8, MDA-MB-231, and HFL-1 cell lines with IC50 values of 0.019 to 0.118 μM. Cell cycle analysis reveals a concentration-dependent increase in G2/M phase arrest, while apoptosis analysis shows a significant rise in apoptotic cells, indicating effective induction of programmed cell death. Additionally, cell migration assays in HUVECs highlight a significant dose-dependent decrease in cell migration, emphasizing its role in inhibiting metastasis-related cellular movements.

Tubulin polymerization-IN-14 (Compound 20a), administered intravenously at 15 and 30 mg/kg daily for 21 days, exhibited a dose-dependent anti-tumor effect in a liver tumor allograft mouse model (Five-week-old male ICR mice), significantly reducing tumor weight by 68.7% at the 30 mg/kg dosage without evident toxicity or significant body weight loss [1].