Thiocolchicine

SKU: orb1303136

Description

Thiocolchicine is a potent tubulin polymerization inhibitor (IC50=2.5 µM, Ki=0.7 µM) that induces apoptotic cell death. It serves as a cytotoxic payload in Antibody-Drug Conjugate (ADC) development and is used in cancer research for both in vitro mechanistic studies and in vivo efficacy models.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 2730-71-4
• MW: 415.5
• Purity: 98.19% (May vary between batches)
• Formula: C₂₂H₂₅NO₅S
• SMILES: COc1cc2CC[C@H](NC(C)=O)c3cc(=O)c(SC)ccc3-c2c(OC)c1OC
• Target: Apoptosis,Microtubule Associated
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.94 mM);DMSO:95 mg/mL (228.64 mM)

Bioactivity

• Target IC50:
  Tubulin polymerization:0.7 µM(Ki)|Tubulin polymerization:2.5 µM
• In Vitro:
  Thiocolchicine (1 nM-100 μM; 24-72 hours) shows a relationship between cell cycle blocking activity and growth inhibition in breast cancer cells. Thiocolchicine inhibits cell proliferation of MDA-MB-231 and multidrug-resistant (MDR) MCF-7 ADRr breast cancer cells with IC50s of 0.6 nM and 400 nM, respectively, as well as MDR CEM-VBL leukemia cells with an IC50 of 50 nM. Thiocolchicine is against MCF-7, LoVo, LoVo/DX, A-549 and BALB/3T3 cells with IC50 values of 0.01 μM, 0.021 μM, 0.398 μM, 0.011 μM and 0.114 μM, respectively.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tubulin polymerization, Thiocolchicine, Inhibitor, MDR-positive, MCF-7, leukemia, inhibit, LoVo, LoVo/DX, Microtubule/Tubulin, Microtubule Associated, MicrotubuleAssociated, Apoptosis, Analogue, cancer, BALB/3T3, A-549, breast, Colchicine

Compound Identifiers

PubChem CID

17648