Cat. No.: HY-121993

Combretastatin A-1

Name: Combretastatin A-1
Brand: MedChemExpress
SKU: HY-121993
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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.

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Pureté : 97.03%
CAS No.: 109971-63-3
Formule: C₁₈H₂₀O₆
Masse moléculaire:332.35

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Combretastatin A-1 Chemical Structure

CAS No.: 109971-63-3

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HY-121993R
Combretastatin A-1 (Standard)

Microtubule Inhibitor

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

Microtubule/Tubulin^[1]

Voir tous les produits spécifiques à Isoform Wnt :

Cellular Effect

Cell Line	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	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	Antitumor activity against human BxPC3 cells by sulforhodamine B assay Antitumor activity against human BxPC3 cells by sulforhodamine B assay	[PMID: 19228038]
BXPC-3	GI₅₀	4.4 μM Compound: CA1, combretastatin A1	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]

In Vitro

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.

Western Blot Analysis^[2]

Cell Line:

HepG2 cells
Concentration:

1, 5, 10 nM
Incubation Time:

24 hours
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.

In Vivo

Combretastatin A-1 (1-4 mg/kg; i.v. every other day for 4 weeks) significantly reduces the tumor volume in HepG2 subcutaneous xenograft model^[2].
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.

Animal Model:

Male athymic BALB/c nu/nu mice (16-18 g; 4-6 weeks old) were inoculated with HepG2 cells^[2]
Dosage:

1, 2, 4 mg/kg
Administration:

I.v. every other day for 4 weeks
Result:

Resulted in a significant tumor volume reduction at the dose of 2 mg/kg or 4 mg/kg.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 109971-63-3
Appearance Solid
Masse moléculaire 332.35
Formule C₁₈H₂₀O₆
Color White to off-white
SMILES

COC1=CC=C(/C=C\C2=CC(OC)=C(C(OC)=C2)OC)C(O)=C1O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

BME Front

Quantifying Spatiotemporal Heterogeneity of Tumor Metabolism and Vasculature with a Multiparametric Point-of-Investigation Microscope. [Abstract]

2025 Dec 9:6:0207. PMID: 41377143

Solvant et solubilité

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0089 mL

15.0444 mL

30.0888 mL

5 mM

0.6018 mL

3.0089 mL

6.0178 mL

10 mM

0.3009 mL

1.5044 mL

3.0089 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

Combretastatin A-1

1 Cited Publications

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Combretastatin A-1

Publications Citing Use of MedChemExpress (MCE) Combretastatin A-1

Voir tous les produits spécifiques à Isoform Wnt