Combretastatin A-1

SKU: orb1693389

Description

Combretastatin A-1 is a potent microtubule-depolymerizing agent with antitumor and anti-angiogenic properties. It inactivates AKT and suppresses the Wnt/β-catenin pathway, making it a valuable tool for studying hepatocellular carcinoma in both in vitro and in vivo models.

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 109971-63-3
• MW: 332.35
• Purity: 97.49%
• Formula: C₁₈H₂₀O₆
• SMILES: COc1ccc(\C=C/c2cc(OC)c(OC)c(OC)c2)c(O)c1O
• Target: Akt,Wnt/beta-catenin,Microtubule Associated
• Solubility: Ethanol:3 mg/mL (9.03 mM);DMSO:PBS (pH 7.2) (1:1):0.5 mg/mL (1.5 mM);DMSO:80 mg/mL (240.71 mM);DMF:5 mg/mL (15.04 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (9.93 mM)

Bioactivity

• Target IC50:
  MDA-MB-231 cells:17.6 nM|Bel-7402 cells:38.4 nM|SMMC-7721 cells:12.8 nM|NCI-1975 cells:256.3 nM|BGC-823 cells:12.2 nM|CT-26:1075 nM|MCF-7 cells:46.0 nM|LM-3:33.8 nM|Huh7 cells:728.2 nM|A375 cells:61 nM|HepG2 cells:9.2 nM|Hepa1-6:32.9 nM
• In Vivo:
  In the HepG2 subcutaneous xenograft model, Combretastatin A-1 (1-4 mg/kg; i.v. every other day for 4 weeks) significantly reduces the tumor volume . In the orthotopic hepatocellular carcinoma mouse model, Combretastatin A-1 (2 mg/kg; every other day for 21 days) demonstrates enhanced apoptosis .
• In Vitro:
  Combretastatin A-1 (CA1P) induces apoptosis of TAMs in vitro through the same mechanism observed in HepG2 cells, and it eliminates TAMs in the tumor microenvironment (TME) in vivo. Combretastatin A-1 (1-10 nM; 24 hours) induces AKT inactivation and removal of GSK-3β inhibition by microtubule depolymerization, leading to HepG2 cell apoptosis . Combretastatin A-1 (1-50 nM; 6 hours) reduces the mitochondrial membrane potential (MMP) of HepG2 cells and induces the accumulation of ROS in a dose-dependent manner .

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Akt, Combretastatin A1, Combretastatin A-1, Combretastatin A 1, microtubule, Microtubule Associated, MicrotubuleAssociated

Compound Identifiers

PubChem CID

5458993