Combretastatin A4

SKU: orb1300975

Description

Combretastatin A4 (CA4) is a potent small molecule that binds to β-tubulin with high affinity (Kd: 0.4 µM), functioning as a microtubule-destabilizing agent. It is widely used in cancer research for its anti-angiogenic and vascular-disrupting properties, applicable in both in vitro cytotoxicity assays and in vivo tumor model studies.

Research Area

Signal Transduction

Key Properties

• CAS Number: 117048-59-6
• MW: 316.35
• Purity: 99.81% (May vary between batches)
• Formula: C₁₈H₂₀O₅
• SMILES: O(C)C1=C(OC)C=C(/C=C\C2=CC(O)=C(OC)C=C2)C=C1OC
• Target: Microtubule Associated
• Solubility: DMSO:250 mg/mL (790.26 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (7.9 mM);Ethanol:31.6 mg/mL (99.89 mM)

Bioactivity

• Target IC50:
  β-tubulin:0.4 μM(Kd)
• In Vivo:
  Combretastatin A4, at a concentration of 1 μM, inhibits microtubule polymerization by 35%, while a concentration of 10 μM nearly completely blocks it. Additionally, Combretastatin A4 effectively inhibits the growth of a variety of cell lines, including MDA-MB-231, Hela, A549, HL-60, SF295, HCT-8, MDA-MB435, OVCAR-8, PC3M, NCI-H358M, and lymphocytes, with respective IC50 values of 2.8, 0.9, 3.8, 2.1, 6.2, 5.3, 7.9, 0.37, 4.7, 8, and 3.2 nM.
• In Vitro:
  In NT2 and MDA-MB-231 breast tumor models, Combretastatin A4 (100 mg/kg, i.p.) significantly reduced lipid R1 levels and decreased pO2 as measured by Electron Paramagnetic Resonance Oxygen Imaging. Additionally, Combretastatin A4 (100 mg/kg, i.p.) notably reduced Ktrans in male NMRI mice.
• Cell Research:
  MDA-MB-231, A549, and HeLa cells are grown in DMEM medium (115 units/mL of penicillin G, 115 μg/mL of streptomycin, and 10% fetal bovine serum). Cells are seeded in 96-well plates (5000 cells/well) containing 50 μL of growth medium for 24 h. After medium removal, 100 μL of fresh medium containing individual analogue compounds at di erent concentrations is added to each well and incubated at 37 ℃ for 72 h. After 24 h of culture, the cells are supplemented with 50 μL of analogue compounds dissolved in DMSO (less than 0.25% in each preparation). After 72 h of incubation, 20 μL of resazurin is added for 2 h before recording uorescence at 560 nm (excitation) and 590 nm (emission) using a Victor microtiter plate uorimeter. The IC50 is de ned as the compound concentration required to inhibit cell proliferation by 50% in comparison with cells treated with the maximum amount of DMSO (0.25%) and considered as 100% viability.(Only for Reference)

Storage & Handling

• Storage: 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

CA 4, CA4, CA-4, Combretastatin A 4, Combretastatin A4, Combretastatin A-4, CRC 87-09, Microtubule Associated, Microtubule/Tubulin, MicrotubuleAssociated, inhibit, Inhibitor, Tubulin β

Compound Identifiers

PubChem CID

5351344