Combretastatin A-1
Based on 1 publication(s) in Google Scholar
Combretastatin A-1 is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 exhibits anti-tumor and anti-vascular effects.
For research use only. We do not sell to patients.
- Purity: 97.03%
- CAS No.: 109971-63-3
- Formula: C18H20O6
- Molecular Weight:332.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Combretastatin A-1
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Biological Activity
Microtubule/Tubulin[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
0.82 μM
Compound: 29; CA1
|
Cytotoxicity against human A549 cells incubated for 4 hrs in anoxic condition followed by oxic exposure for 48 hrs by sulforhodamine B assay
Cytotoxicity against human A549 cells incubated for 4 hrs in anoxic condition followed by oxic exposure for 48 hrs by sulforhodamine B assay
|
[PMID: 32196334] |
| A549 | GI50 |
1.2 μM
Compound: 29; CA1
|
Cytotoxicity against human A549 cells incubated for 52 hrs in oxic condition by sulforhodamine B assay
Cytotoxicity against human A549 cells incubated for 52 hrs in oxic condition by sulforhodamine B assay
|
[PMID: 32196334] |
| BXPC-3 | GI50 |
4.4 μg/mL
Compound: 2a
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Cytotoxicity against human BxPC3 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human BxPC3 cells after 48 hrs by sulforhodamine B assay
|
[PMID: 16252907] |
| BXPC-3 | GI50 |
4.4 μg/mL
Compound: 4, CA1
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Antitumor activity against human BxPC3 cells by sulforhodamine B assay
Antitumor activity against human BxPC3 cells by sulforhodamine B assay
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[PMID: 19228038] |
| BXPC-3 | GI50 |
4.4 μM
Compound: CA1, combretastatin A1
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Cytotoxicity against human BXPC3 cells after 48 hrs by SRB assay
Cytotoxicity against human BXPC3 cells after 48 hrs by SRB assay
|
[PMID: 18303849] |
| BXPC-3 | GI50 |
4.4 μg/mL
Compound: 3a
|
Evaluated for growth inhibition (anticancer activity) of human pancreas-a BXPC-3 cell line.
Evaluated for growth inhibition (anticancer activity) of human pancreas-a BXPC-3 cell line.
|
[PMID: 10893310] |
| CCRF-CEM | IC50 |
>100 μM
Compound: 1, CA-1
|
Cytotoxicity against human CEM cells by alamar blue assay
Cytotoxicity against human CEM cells by alamar blue assay
|
[PMID: 22137934] |
| DU-145 | GI50 |
0.013 μM
Compound: 2, CA1
|
Cytotoxicity against human DU145 cells by SRB assay
Cytotoxicity against human DU145 cells by SRB assay
|
[PMID: 20496923] |
| DU-145 | GI50 |
0.0326 μM
Compound: CA1 (Z)
|
Cytotoxicity against human DU145 cells by SRB assay
Cytotoxicity against human DU145 cells by SRB assay
|
[PMID: 21718055] |
| DU-145 | GI50 |
0.033 μM
Compound: CA1
|
Growth inhibition of human DU145 cells by sulforhodamine B assay
Growth inhibition of human DU145 cells by sulforhodamine B assay
|
[PMID: 23772309] |
| DU-145 | GI50 |
0.17 μg/mL
Compound: 2a
|
Cytotoxicity against human DU145 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human DU145 cells after 48 hrs by sulforhodamine B assay
|
[PMID: 16252907] |
| DU-145 | GI50 |
0.17 μg/mL
Compound: 4, CA1
|
Antitumor activity against human DU145 cells by sulforhodamine B assay
Antitumor activity against human DU145 cells by sulforhodamine B assay
|
[PMID: 19228038] |
| DU-145 | GI50 |
0.17 μM
Compound: CA1, combretastatin A1
|
Cytotoxicity against human DU145 cells after 48 hrs by SRB assay
Cytotoxicity against human DU145 cells after 48 hrs by SRB assay
|
[PMID: 18303849] |
| DU-145 | GI50 |
0.17 μg/mL
Compound: 3a
|
Evaluated for growth inhibition (anticancer activity) of Human prostate cancer DU-145 cell line
Evaluated for growth inhibition (anticancer activity) of Human prostate cancer DU-145 cell line
|
[PMID: 10893310] |
| DU-145 | GI50 |
0.51 μM
Compound: CA1
|
Growth inhibition of human DU145 after 48 hrs by SRB assay
Growth inhibition of human DU145 after 48 hrs by SRB assay
|
[PMID: 18722127] |
| FaDu | GI50 |
0.23 μg/mL
Compound: 1a
|
Cytotoxicity against human FaDu cells
Cytotoxicity against human FaDu cells
|
[PMID: 10924176] |
| Fibroblast | IC50 |
>100 μM
Compound: 1, CA-1
|
Cytotoxicity against human fibroblast cells by alamar blue assay
Cytotoxicity against human fibroblast cells by alamar blue assay
|
[PMID: 22137934] |
| HT-29 | IC50 |
0.9 μM
Compound: 1, CA-1
|
Cytotoxicity against human HT-29 cells by alamar blue assay
Cytotoxicity against human HT-29 cells by alamar blue assay
|
[PMID: 22137934] |
| HUVEC | IC50 |
2.6 nM
Compound: 3, CA-1
|
Antivascular activity against HUVEC cells assessed as cell growth inhibition after 24 hrs by xCELLigence assay
Antivascular activity against HUVEC cells assessed as cell growth inhibition after 24 hrs by xCELLigence assay
|
[PMID: 22304851] |
| HUVEC | IC50 |
4.1 nM
Compound: 3, CA-1
|
Antivascular activity against HUVEC cells assessed as cell growth inhibition after 48 hrs by xCELLigence assay
Antivascular activity against HUVEC cells assessed as cell growth inhibition after 48 hrs by xCELLigence assay
|
[PMID: 22304851] |
| KM-20L2 | GI50 |
0.061 μg/mL
Compound: 2a
|
Cytotoxicity against human KM20L2 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human KM20L2 cells after 48 hrs by sulforhodamine B assay
|
[PMID: 16252907] |
| KM-20L2 | GI50 |
0.061 μM
Compound: CA1, combretastatin A1
|
Cytotoxicity against human KM20L2 cells after 48 hrs by SRB assay
Cytotoxicity against human KM20L2 cells after 48 hrs by SRB assay
|
[PMID: 18303849] |
| KM-20L2 | GI50 |
0.061 μg/mL
Compound: 3a
|
Evaluated for growth inhibition (anticancer activity) of Human colon KM20L2 cancer cell line
Evaluated for growth inhibition (anticancer activity) of Human colon KM20L2 cancer cell line
|
[PMID: 10893310] |
| L1210 | IC50 |
0.6 μM
Compound: Combretastatin A-1
|
Cytotoxicity against mouse L1210 cells after 24 hrs
Cytotoxicity against mouse L1210 cells after 24 hrs
|
[PMID: 3404149] |
| MCF7 | IC50 |
75.9 μM
Compound: 1, CA-1
|
Cytotoxicity against human MCF7 cells by alamar blue assay
Cytotoxicity against human MCF7 cells by alamar blue assay
|
[PMID: 22137934] |
| NCI-H460 | GI50 |
0.015 μM
Compound: CA1
|
Growth inhibition of human NCI-H460 cells by sulforhodamine B assay
Growth inhibition of human NCI-H460 cells by sulforhodamine B assay
|
[PMID: 23772309] |
| NCI-H460 | GI50 |
0.0153 μM
Compound: CA1 (Z)
|
Cytotoxicity against human NCI-H460 cells by SRB assay
Cytotoxicity against human NCI-H460 cells by SRB assay
|
[PMID: 21718055] |
| NCI-H460 | GI50 |
0.046 μM
Compound: 2, CA1
|
Cytotoxicity against human NCI-H460 cells by SRB assay
Cytotoxicity against human NCI-H460 cells by SRB assay
|
[PMID: 20496923] |
| NCI-H460 | GI50 |
0.74 μg/mL
Compound: 2a
|
Cytotoxicity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay
|
[PMID: 16252907] |
| NCI-H460 | GI50 |
0.74 μg/mL
Compound: 4, CA1
|
Antitumor activity against human NCI-H460 cells by sulforhodamine B assay
Antitumor activity against human NCI-H460 cells by sulforhodamine B assay
|
[PMID: 19228038] |
| NCI-H460 | GI50 |
0.74 μM
Compound: CA1, combretastatin A1
|
Cytotoxicity against human NCIH460 cells after 48 hrs by SRB assay
Cytotoxicity against human NCIH460 cells after 48 hrs by SRB assay
|
[PMID: 18303849] |
| NCI-H460 | GI50 |
0.74 μg/mL
Compound: 3a
|
Evaluated for growth inhibition (anticancer activity) of Human CNS cancer SF-295 cell line
Evaluated for growth inhibition (anticancer activity) of Human CNS cancer SF-295 cell line
|
[PMID: 10893310] |
| NCI-H460 | GI50 |
2.2 μM
Compound: CA1
|
Growth inhibition of human NCI-H460 after 48 hrs by SRB assay
Growth inhibition of human NCI-H460 after 48 hrs by SRB assay
|
[PMID: 18722127] |
| NCI-H460 | IC50 |
1.8 μM
Compound: 1, CA-1
|
Cytotoxicity against human NCI-H460 cells by alamar blue assay
Cytotoxicity against human NCI-H460 cells by alamar blue assay
|
[PMID: 22137934] |
| P388 | ED50 |
0.2 μg/mL
Compound: 1a
|
Cytotoxicity against mouse P388 cells
Cytotoxicity against mouse P388 cells
|
[PMID: 10924176] |
| P388 | ED50 |
0.251 μg/mL
Compound: 2a
|
Cytotoxicity against mouse P388 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against mouse P388 cells after 48 hrs by sulforhodamine B assay
|
[PMID: 16252907] |
| P388 | ED50 |
0.3 μg/mL
Compound: 4, CA1
|
In vivo antitumor activity against mouse P388 cells
In vivo antitumor activity against mouse P388 cells
|
[PMID: 19228038] |
| P388 | ED50 |
0.99 μg/mL
Compound: 1a, NSC-600032
|
In vivo cytotoxicity against mouse P388 cells
In vivo cytotoxicity against mouse P388 cells
|
[PMID: 3598594] |
| P388 | GI50 |
0.3 μg/mL
Compound: 3a
|
Evaluated for growth inhibition (anticancer activity) of Murine P388 lymphocytic leukemia cell line
Evaluated for growth inhibition (anticancer activity) of Murine P388 lymphocytic leukemia cell line
|
[PMID: 10893310] |
| Panel (Carcinoma cell lines) | GI50 |
1.62 x 10-8M
Compound: 2e
|
In vitro antitumor activity against human tumor cancer cell lines
In vitro antitumor activity against human tumor cancer cell lines
|
[PMID: 7752190] |
| Pituitary gland cell | IC50 |
0.63 nM
Compound: Combretastatin
|
Inhibitory activity against GHRH-stimulated GH release from monolayer cultures of rat pituitary cells
Inhibitory activity against GHRH-stimulated GH release from monolayer cultures of rat pituitary cells
|
[PMID: 12617894] |
| Platelet | IC50 |
60.58 μg
Compound: 9, combretastatin A-1
|
Inhibition of adenosine diphosphate-induced platelet aggregation in human platelet-rich plasma
Inhibition of adenosine diphosphate-induced platelet aggregation in human platelet-rich plasma
|
[PMID: 9392877] |
| Platelet | IC50 |
68.5 μg
Compound: 9, combretastatin A-1
|
Inhibition of collagen-induced platelet aggregation in human platelet-rich plasma
Inhibition of collagen-induced platelet aggregation in human platelet-rich plasma
|
[PMID: 9392877] |
| SK-OV-3 | GI50 |
0.038 μM
Compound: CA1
|
Growth inhibition of human SKOV3 cells by sulforhodamine B assay
Growth inhibition of human SKOV3 cells by sulforhodamine B assay
|
[PMID: 23772309] |
| SK-OV-3 | GI50 |
0.0384 μM
Compound: CA1 (Z)
|
Cytotoxicity against human SKOV3 cells by SRB assay
Cytotoxicity against human SKOV3 cells by SRB assay
|
[PMID: 21718055] |
Combretastatin A-1 (72 h) inhibits the growth of various tumor cell lines in vitro, including HepG2, SMMC-7721, Hepa 1-6, LM-3, Bel-7402, Huh7, BGC-803, MDA-MB-231, MCF-7, A375, NCI-1975, CT-26, HT-29, A549 cells (IC50=9.2, 12.8, 32.9, 33.8, 38.4, 728.2, 12.2, 17.6, 46.0, 61.0, 256.3, 1075.0, 2082.0, 2247.0 nM, respectively)[2].
Combretastatin A-1 (1-10 nM; 24 h) induces apoptosis by microtubule depolymerization-induced AKT inactivation and the removal of GSK-3β inhibition in HepG2 cells[2].
Combretastatin A-1 (1-50 nM; 6 h) decreases the mitochondrial membrane potential (MMP) of HepG2 cells. Combretastatin A-1 shows dose-dependently ROS accumulation in HepG2 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:1, 5, 10 nM
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Incubation Time:24 hours
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Result:Significantly decreased Mcl-1 expression, but the Bcl-2 level was unchanged.
Reduced p-GSK 3β (Ser9) without altering total GSK-3β protein levels, indicating an activation of GSK-3β.
Reduced AKT phosphorylation on Ser473 without an obvious change in the total AKT protein levels.
Combretastatin A-1 (2 mg/kg; every other day for 21 days) shows enhanced apoptosis in orthotopic hepatocellular carcinoma mouse model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male athymic BALB/c nu/nu mice (16-18 g; 4-6 weeks old) were inoculated with HepG2 cells[2]
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Dosage:1, 2, 4 mg/kg
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Administration:I.v. every other day for 4 weeks
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Result:Resulted in a significant tumor volume reduction at the dose of 2 mg/kg or 4 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 109971-63-3
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Appearance Solid
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Molecular Weight 332.35
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Formula C18H20O6
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Color White to off-white
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SMILES
COC1=CC=C(/C=C\C2=CC(OC)=C(C(OC)=C2)OC)C(O)=C1O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : ≥ 100 mg/mL (300.89 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.26 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.26 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Pettit GR, et, al. Isolation, structure, and synthesis of combretastatins A-1 and B-1, potent new inhibitors of microtubule assembly, derived from Combretum caffrum. J Nat Prod. Jan-Feb 1987;50(1):119-31. [Content Brief]
[2]. Mao J, et, al. Combretastatin A-1 phosphate, a microtubule inhibitor, acts on both hepatocellular carcinoma cells and tumor-associated macrophages by inhibiting the Wnt/β-catenin pathway. Cancer Lett. 2016 Sep 28;380(1):134-43. [Content Brief]
[3]. Holwell SE, et, al. Anti-tumor and anti-vascular effects of the novel tubulin-binding agent combretastatin A-1 phosphate. Anticancer Res. Nov-Dec 2002;22(6C):3933-40. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0089 mL | 15.0444 mL | 30.0888 mL | 75.2219 mL |
| 5 mM | 0.6018 mL | 3.0089 mL | 6.0178 mL | 15.0444 mL | |
| 10 mM | 0.3009 mL | 1.5044 mL | 3.0089 mL | 7.5222 mL | |
| 15 mM | 0.2006 mL | 1.0030 mL | 2.0059 mL | 5.0148 mL | |
| 20 mM | 0.1504 mL | 0.7522 mL | 1.5044 mL | 3.7611 mL | |
| 25 mM | 0.1204 mL | 0.6018 mL | 1.2036 mL | 3.0089 mL | |
| 30 mM | 0.1003 mL | 0.5015 mL | 1.0030 mL | 2.5074 mL | |
| 40 mM | 0.0752 mL | 0.3761 mL | 0.7522 mL | 1.8805 mL | |
| 50 mM | 0.0602 mL | 0.3009 mL | 0.6018 mL | 1.5044 mL | |
| 60 mM | 0.0501 mL | 0.2507 mL | 0.5015 mL | 1.2537 mL | |
| 80 mM | 0.0376 mL | 0.1881 mL | 0.3761 mL | 0.9403 mL | |
| 100 mM | 0.0301 mL | 0.1504 mL | 0.3009 mL | 0.7522 mL |