Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a Pd-mediated tubulin polymerization inhibitor prodrug. Tubulin Polymerization-IN-1 prodrug is based on colchicine binding site inhibitors (CBSIs) and is developed by reducing toxicity and improving targeted release performance. Compared with the parent compound, the cytotoxicity of Tubulin Polymerization-IN-1 prodrug was reduced by 68.3 times, but its cytotoxicity could be restored in situ in the presence of Pd resin. Mechanistic studies have shown that its antitumor activity is the same as that of CBSIs. In in vivo experiments, Tubulin Polymerization-IN-1 prodrug significantly inhibited tumor growth after activation with Pd resin (inhibition rate 63.2%). Tubulin Polymerization-IN-1 prodrug is expected to be used in research in the field of anti-cancer.

Physicochemical Properties

Molecular Formula	C22H23FN2O4
Molecular Weight	398.43
CAS #	3033099-32-7
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

References

[1]. 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.

Solubility Data

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.5099 mL	12.5493 mL	25.0985 mL
	5 mM	0.5020 mL	2.5099 mL	5.0197 mL
	10 mM	0.2510 mL	1.2549 mL	2.5099 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.