Bioactivity | Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a palladium (Pd)-mediated tubulin polymerization inhibitor prodrug. Developed based on colchicine binding site inhibitors (CBSIs), it reduces toxicity and enhances targeted release properties. Compared to the parent compound, Tubulin Polymerization-IN-1 prodrug exhibited 68.3-fold lower cytotoxicity, which can be restored in situ in the presence of Pd resin. Mechanistic studies showed that its anticancer activity is consistent with CBSIs. In vivo, Tubulin Polymerization-IN-1 prodrug significantly inhibited tumor growth (63.2%) when activated by Pd resin. It holds promise for research in the field of anticancer therapy[1]. |
CAS | 3033099-32-7 |
Formula | C22H23FN2O4 |
Molar Mass | 398.43 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Li J, et al. Palladium-Mediated Bioorthogonal System for Prodrug Activation of N-Benzylbenzamide-Containing Tubulin Polymerization Inhibitors for the Treatment of Solid Tumors. J Med Chem. 2024 Nov 14;67(21):19905-19924. |