2. Apoptosis Cell Cycle/DNA Damage
  3. Caspase Apoptosis Topoisomerase
  4. Phenoxodiol

Phenoxodiol  (Synonyms: Idronoxil; Dehydroequol; Haginin E)

Cat. No.: HY-13721 Purity: 99.76%
COA Handling Instructions

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Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner.

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Phenoxodiol Chemical Structure

Phenoxodiol Chemical Structure

CAS No. : 81267-65-4

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Phenoxodiol Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Phenoxodiol

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Description

Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner[1][2].

IC50 & Target

Caspase, DNA topoisomerase II[1][2].
In Vitro

Phenoxodiol (Idronoxil) (0-10 μg/mL; 24 h) decreases cell viability of primary ovarian cancer cells[1].
Phenoxodiol (0-10 μg/mL; 24 h) induces apoptosis and restores sensitivity to Fas-mediated apoptosis in ovarian cancer cells[1].
Phenoxodiol (0-10 μg/mL; 24 h) induces caspase-8 activation and FLIP downregulation through the Akt-pathway. Phenoxodiol-induced apoptosis involves activation of the mitochondrial pathway and is caspase dependent. Phenoxodiol treatment results in downregulation and cleavage of XIAP[1].
Phenoxodiol (10 and 30 μM; 24 and 48 h) induces cell cycle arrest in the G1/S phase of the cell cycle in prostate cancer cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Phenoxodiol Related Antibodies

Cell Viability Assay[1]

Cell Line: R182s, R127, Hey, CP70, A2780, R187, R188, R207 and OSE cells
Concentration: 0, 0.01, 0.1, 1 and 10 μg/mL
Incubation Time: 24 h
Result: A significant decrease in cell viabilityin all the ovarian cancer cell cultures was observed at a concentration of 10 μg/mL (41.6 μM) and did not affect ovarian surface epithelial (OSE) cells’ viability. In CP70 cells, the IC50 was 1.35 μM.

Apoptosis Analysis[1]

Cell Line: CP70 and OSE cells
Concentration: 10 μg/mL
Incubation Time: 24 h
Result: Induced apoptosis and resulted in a twofold increase in caspase-3 activity. No change in caspase-3 activity was found in normal OSE cells.

Western Blot Analysis[1]

Cell Line: Ovarian cancer cells
Concentration: 10 μg/mL
Incubation Time: 24 h
Result: Induced caspase-8 activation, characterized bycleavage of procaspase-8 into its p43/41 and p28 forms and in downregulation of the p43 form of FLIPC in all the primarycultures as well as in the CP70 and Hey cell lines. Decreased the levels of Akt expression. Resulted in XIAP downregulation and cleavage to its 30 kDa inactive form.

Cell Cycle Analysis[2]

Cell Line: LNCaP, DU145 and PC3 cells
Concentration: 10 and 30 μM
Incubation Time: 24 and 48 h
Result: Induced significantly decreased G2 phase cell populations versus DMSO vehicle control, over 24 hours for both 10 μM and 30 μM treatments. The S phase cell population was found to increase versus DMSO vehicle control.

RT-PCR[2]

Cell Line: LNCaP, DU145 and PC3 cells
Concentration: 10 and 30 μM
Incubation Time: 24 and 48 h
Result: PC3 cells were found to significantly increase the expression of c-Myc at 30 μM after 48 h. Decreased the expression of Cyclin-D1 after 24 hours of treatment with 30 μM in DU145 and PC3 cells. Decreased the expression of Ki-67 after 24 hours of treatment with 10 and 30 μM in LNCaP and PC3 cells. Increased the expression of p21 in LNCaP and PC3 cells.
Clinical Trial
Molecular Weight

240.25

Formula

C15H12O3
CAS No.
Appearance

Solid

Color

Off-white to brown

SMILES

OC1=CC=C2C=C(C3=CC=C(O)C=C3)COC2=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (416.23 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1623 mL 20.8117 mL 41.6233 mL
5 mM 0.8325 mL 4.1623 mL 8.3247 mL
View the 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.

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (10.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (10.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.76%

COA (245 KB) HNMR (231 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References

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 4.1623 mL 20.8117 mL 41.6233 mL 104.0583 mL
5 mM 0.8325 mL 4.1623 mL 8.3247 mL 20.8117 mL
10 mM 0.4162 mL 2.0812 mL 4.1623 mL 10.4058 mL
15 mM 0.2775 mL 1.3874 mL 2.7749 mL 6.9372 mL
20 mM 0.2081 mL 1.0406 mL 2.0812 mL 5.2029 mL
25 mM 0.1665 mL 0.8325 mL 1.6649 mL 4.1623 mL
30 mM 0.1387 mL 0.6937 mL 1.3874 mL 3.4686 mL
40 mM 0.1041 mL 0.5203 mL 1.0406 mL 2.6015 mL
50 mM 0.0832 mL 0.4162 mL 0.8325 mL 2.0812 mL
60 mM 0.0694 mL 0.3469 mL 0.6937 mL 1.7343 mL
80 mM 0.0520 mL 0.2601 mL 0.5203 mL 1.3007 mL
100 mM 0.0416 mL 0.2081 mL 0.4162 mL 1.0406 mL
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Phenoxodiol Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Phenoxodiol81267-65-4Idronoxil Dehydroequol Haginin ECaspaseApoptosisTopoisomeraseovarian cancerCP70prostate cancerXIAPInhibitorinhibitorinhibit

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