Phenoxodiol (Haginin E)

For research use only.

Catalog No.S9634 Synonyms: Idronoxil, Dehydroequol, NV 06, PXD

Phenoxodiol (Haginin E) Chemical Structure

CAS No. 81267-65-4

Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.

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Biological Activity

Description Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.
Targets
Caspase [1]
()
XIAP [1]
()
FLIP [1]
()
Topo II [2]
()
In vitro

Primary ovarian cancer cells, isolated from ascitic fluids of ovarian cancer patients, resistant to conventional chemotherapy, undergo apoptosis following phenoxodiol treatment. This effect is dependent upon the activation of the caspase system, inhibiting XIAP, an inhibitor of apoptosis, and disrupting FLICE inhibitory protein (FLIP) expression through the Akt signal transduction pathway. Phenoxodiol is an efficient inducer of cell death in ovarian cancer cells and sensitizes the cancer cells to Fas-mediated apoptosis.[1]

In vivo

In an in vivo colon cancer model, Balb/C mice administered low-dose Phenoxodiol (PXD), exhibits significantly reduced tumour growth rates and prolonged survival (in 40% of the animals).[4]

Protocol

Cell Research:

[1]

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  • Cell lines: primary ovarian cancer cells
  • Concentrations: 0.1 μg/ml, 1 μg/ml, 10 μg/ml
  • Incubation Time: 24 h
  • Method:

    Cells are treated in the presence or absence of 500 ng/ml Fas-antibody in Optimem for 24 h or with 0.1, 1 or 10 μg/ml phenoxodiol, NV03, NV05 or NV07 in Optimem for 24 h. For treatment with phenoxodiol and caspase inhibitors, 10 μg/ml phenoxodiol is used alone, or in combination with 20 μM general caspase-inhibitor Z-VADFMK and incubated for 24 h.


    (Only for Reference)
Animal Research:

[4]

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  • Animal Models: 7–8-week-old female Balb/C mice
  • Dosages: 10 mg/kg, 20 mg/kg
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 48 mg/mL (199.79 mM)
Ethanol 48 mg/mL (199.79 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 240.25
Formula

C15H12O3

CAS No. 81267-65-4
Storage powder
in solvent
Synonyms Idronoxil, Dehydroequol, NV 06, PXD
Smiles C1C(=CC2=C(O1)C=C(C=C2)O)C3=CC=C(C=C3)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04957290 Not yet recruiting Drug: NOX66|Radiation: EBRT Metastatic Castration-resistant Prostate Cancer and Other Solid Tumors Noxopharm Limited August 17 2021 Phase 1|Phase 2
NCT00557037 Completed Drug: Phenoxodiol Prostate Cancer MEI Pharma Inc. November 2007 Phase 2
NCT00878800 Completed Drug: PXD101|Drug: Doxorubicin Dose Escalation: Solid Tumors|MTD: Soft Tissue Sarcomas Onxeo|Spectrum Pharmaceuticals Inc December 2006 Phase 1|Phase 2
NCT00413075 Completed Drug: oral belinostat Solid Tumor|Lymphoma Onxeo|Spectrum Pharmaceuticals Inc June 2006 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID