Combretastatin A-1 phosphate tetrasodium
Combretastatin A-1 phosphate (OXi-4503) tetrasodium, a proagent of Combretastatin A-1, is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 phosphate tetrasodium inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 phosphate tetrasodium exhibits anti-tumor and anti-vascular effects.
For research use only. We do not sell to patients.
- CAS No.: 288847-34-7
- Formula: C18H18Na4O12P2
- Molecular Weight:580.23
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Microtubule/Tubulin[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BXPC-3 | GI50 |
>10 μg/mL
Compound: CA1P
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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 |
1.5 μg/mL
Compound: 2b
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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
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[PMID: 16252907] |
| BXPC-3 | GI50 |
1.5 μg/mL
Compound: 3e
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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.
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[PMID: 10893310] |
| DU-145 | GI50 |
0.034 μg/mL
Compound: 2b
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Cytotoxicity against human DU145 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human DU145 cells after 48 hrs by sulforhodamine B assay
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[PMID: 16252907] |
| DU-145 | GI50 |
0.034 μg/mL
Compound: 3e
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Evaluated for growth inhibition (anticancer activity) in Human prostate cancer DU-145 cell line
Evaluated for growth inhibition (anticancer activity) in Human prostate cancer DU-145 cell line
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[PMID: 10893310] |
| DU-145 | GI50 |
2.7 μg/mL
Compound: CA1P
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Antitumor activity against human DU145 cells by sulforhodamine B assay
Antitumor activity against human DU145 cells by sulforhodamine B assay
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[PMID: 19228038] |
| KM-20L2 | GI50 |
>10 μg/mL
Compound: CA1P
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Antitumor activity against human KM20L2 cells by sulforhodamine B assay
Antitumor activity against human KM20L2 cells by sulforhodamine B assay
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[PMID: 19228038] |
| KM-20L2 | GI50 |
0.53 μg/mL
Compound: 2b
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Cytotoxicity against human KM20L2 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human KM20L2 cells after 48 hrs by sulforhodamine B assay
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[PMID: 16252907] |
| MCF7 | GI50 |
0.024 μg/mL
Compound: 2b
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Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay
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[PMID: 16252907] |
| NCI-H460 | GI50 |
0.038 μg/mL
Compound: 2b
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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
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[PMID: 16252907] |
| NCI-H460 | GI50 |
0.038 μg/mL
Compound: 3e
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Evaluated for growth inhibition (anticancer activity) of Human lung-NSC cancer NCI-H460 cell line
Evaluated for growth inhibition (anticancer activity) of Human lung-NSC cancer NCI-H460 cell line
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[PMID: 10893310] |
| NCI-H460 | GI50 |
3.3 μg/mL
Compound: CA1P
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Antitumor activity against human NCI-H460 cells by sulforhodamine B assay
Antitumor activity against human NCI-H460 cells by sulforhodamine B assay
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[PMID: 19228038] |
| P388 | ED50 |
<0.01 μg/mL
Compound: 2b
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Cytotoxicity against mouse P388 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against mouse P388 cells after 48 hrs by sulforhodamine B assay
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[PMID: 16252907] |
| P388 | ED50 |
<0.01 μg/mL
Compound: 1d
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Cytotoxicity against mouse P388 cells
Cytotoxicity against mouse P388 cells
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[PMID: 10924176] |
| P388 | ED50 |
<0.01 μM
Compound: CA1P, Oxi4503
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Growth inhibition of mouse P388 cells
Growth inhibition of mouse P388 cells
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[PMID: 18303849] |
| P388 | ED50 |
0.3 μg/mL
Compound: CA1P
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In vivo antitumor activity against mouse P388 cells
In vivo antitumor activity against mouse P388 cells
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[PMID: 19228038] |
| P388 | GI50 |
<0.01 μg/mL
Compound: 3e
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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
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[PMID: 10893310] |
| SF-268 | GI50 |
0.036 μg/mL
Compound: 2b
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Cytotoxicity against human SF268 cells after 48 hrs by sulforhodamine B assay
Cytotoxicity against human SF268 cells after 48 hrs by sulforhodamine B assay
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[PMID: 16252907] |
| SF-295 | GI50 |
0.036 μg/mL
Compound: 3e
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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
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[PMID: 10893310] |
Combretastatin A-1 phosphate (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 phosphate (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 phosphate (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 phosphate (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
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 288847-34-7
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Molecular Weight 580.23
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Formula C18H18Na4O12P2
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SMILES
O=P(O[Na])(O[Na])OC1=C(C(OC)=CC=C1/C=C\C2=CC(OC)=C(C(OC)=C2)OC)OP(O[Na])(O[Na])=O
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Synonyms
OXi-4503 tetrasodium
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Stratford MRL, et, al. Quantitative determination of the anticancer prodrug combretastatin A1 phosphate (OXi4503, CA1P), the active CA1 and its glucuronide metabolites in human urine and of CA1 in plasma by HPLC with mass spectrometric detection. J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Jun 1;898:1-6. [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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Combretastatin A-1 phosphate tetrasodium Related Classifications
HY-16146 Related Classifications
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