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Signaling Pathway

Combretastatin A4

HY-N2146

(CRC 87-09)

Combretastatin A4

Combretastatin A4 Chemical Structure

Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.

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Product name: Combretastatin A4
Cat. No.: HY-N2146

Combretastatin A4 Data Sheet

Related Compound Libraries

Biological Activity of Combretastatin A4

Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.
Kd: 0.4 μM (β-tubulin)
Target: β-tubulin
In vitro: Combretastatin A4 phosphate (≥ 50 μM) significantly increases the percentage of annexin-V-binding cells and significantly decreases forward scatter. Combretastatin A4 phosphate does not appreciably increase hemolysis. Hundred μM Combretastatin A4 phosphate significantly increases Fluo3-fluorescence. The effect of Combretastatin A4 phosphate (100 μM) on annexin-V-binding is significantly blunted, but not abolished, by removal of extracellular Ca2+. Combretastatin A4 phosphate (≥ 50 μM) significantly decreases GSH abundance and ATP levels but does not significantly increase ROS or ceramide[2]. Pretreatment with Combretastatin A4 phosphate does not influence the amount of VM in 3-D culture as well as the expression of these key molecules[4].  
In vivo: DBP and MBP at 30 minutes after administration are higher in rats treated with Combretastatin A4 disodium phosphate 120 mg/10 mL/kg. The toxicokinetic parameters of Combretastatin A4 phosphate and Combretastatin A4 in rats treated with Combretastatin A4 disodium phosphate 120 mg/10 mL/kg are indicated, and the values of Cmax, T1/2, and AUC0-inf for Combretastatin A4 are 156 ± 13 μM, 5.87 ± 1.69 h, and 89.4 ± 10.1 h·μM, respectively[1]. In vivo, W256 tumors show marked intratumoral hypoxia after Combretastatin A4 phosphate treatment, accompanied by increased VM formation. Combretastatin A4 phosphate exhibits only a delay in tumor growth within 2 days but rapid tumor regrowth afterward. VM density is positively related to tumor volume and tumor weight at day 8. Combretastatin A4 phosphate causes hypoxia which induces VM formation in W256 tumors through HIF-1α/EphA2/PI3K/matrix metalloproteinase (MMP) signaling pathway, resulting in the consequent regrowth of the damaged tumor[4].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 316.35 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C₁₈H₂₀O₅
CAS No 117048-59-6
Solvent & Solubility

10 mM in DMSO

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 3.1611 mL 15.8053 mL 31.6106 mL
5 mM 0.6322 mL 3.1611 mL 6.3221 mL
10 mM 0.3161 mL 1.5805 mL 3.1611 mL

References on Combretastatin A4

Inhibitor Kit

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