Phenoxodiol (Haginin E)

Catalog No.S9634 Batch:S963401

Technical Data

Formula	C₁₅H₁₂O₃
Molecular Weight	240.25	CAS No.	81267-65-4
Solubility (25°C)*	In vitro	DMSO	48 mg/mL (199.79 mM)
		Ethanol	48 mg/mL (199.79 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[4]}	Animal Models 7–8-week-old female Balb/C mice Dosages 10 mg/kg, 20 mg/kg Administration IP

Cell Assay:^{^[1]}

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.

Animal Study:^{^[4]}

Animal Models
7–8-week-old female Balb/C mice
Dosages
10 mg/kg, 20 mg/kg
Administration
IP

References

[4] Sylvianna Georgaki, et al. J Cell Mol Med. 2009 Sep;13(9B):3929-38.

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Selleck's Phenoxodiol (Haginin E) has been cited by 1 publication

Evaluation of therapeutic potential of phenoxodiol, a novel isoflavone analog, in renal cancer cells [ Anticancer Res, 2018, 38(10):5709-5716]	PubMed: 30275191

Evaluation of therapeutic potential of phenoxodiol, a novel isoflavone analog, in renal cancer cells [ Anticancer Res, 2018, 38(10):5709-5716]

PubMed: 30275191

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