Thiocolchicine-d3

Thiocolchicine-d3 is deuterium labeled Thiocolchicine. Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 µM) and competitively binds to tubulin with a Ki of 0.7 µM. Thiocolchicine induces cell apoptosis[1][2]. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Klaus M.Hahn, et al. Structural requirements for the binding of colchicine analogs to tubulin: the role of the C-10 substituent. Bioorganic & Medicinal Chemistry Letters.Volume 1, Issue 9, 1991, Pages 471-476

[3]. R De Vincenzo, et al. Antiproliferative Activity of Colchicine Analogues on MDR-positive and MDR-negative Human Cancer Cell Lines. Anticancer Drug Des. 1998 Jan;13(1):19-33.