research use only

Phenoxodiol (Haginin E) Caspase activator

Name: Phenoxodiol (Haginin E)
Brand: Selleck Chemicals
SKU: S9634
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S9634

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

Chemical Structure

Molecular Weight: 240.25

Jump to

Quality Control

Batch: S963401 DMSO]48 mg/mL]false]Ethanol]48 mg/mL]false]Water]Insoluble]false Purity: 99.99%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.99

Related Targets	Bcl-2 PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas
Other Caspase Inhibitors	Emricasan (IDN-6556) Z-VAD-FMK Q-VD-Oph Z-DEVD-FMK Belnacasan (VX-765) Z-IETD-FMK Ac-DEVD-CHO Z-LEHD-FMK TFA Z-VAD(OH)-FMK PAC-1

Solubility

In vitro
Batch:

DMSO : 48 mg/mL (199.79 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 48 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	240.25	Formula	C₁₅H₁₂O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	81267-65-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Idronoxil, Dehydroequol, NV 06, PXD			Smiles	C1C(=CC2=C(O1)C=C(C=C2)O)C3=CC=C(C=C3)O

Mechanism of Action

Targets/IC₅₀/Ki	Caspase XIAP FLIP Topo II
In vitro	Primary ovarian cancer cells, isolated from ascitic fluids of ovarian cancer patients, resistant to conventional chemotherapy, undergo apoptosis following treatment with phenoxodiol (Haginin E). 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. It is an efficient inducer of cell death in ovarian cancer cells and sensitizes the cancer cells to Fas-mediated apoptosis.
In vivo	In an in vivo colon cancer model, Balb/C mice administered low-dose Phenoxodiol (Haginin E) exhibited significantly reduced tumour growth rates and prolonged survival (in 40% of the animals).
References	[1] https://pubmed.ncbi.nlm.nih.gov/12730675/ [2] https://pubmed.ncbi.nlm.nih.gov/12529967/ [3] https://pubmed.ncbi.nlm.nih.gov/16507219/ [4] https://pubmed.ncbi.nlm.nih.gov/19220577/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05100628	Terminated	Metastatic Soft-tissue Sarcoma	Noxopharm Limited	February 11 2022	Phase 1
NCT04957290	Terminated	Metastatic Castration-resistant Prostate Cancer and Other Solid Tumors	Noxopharm Limited	October 25 2021	Phase 1\|Phase 2
NCT00557037	Completed	Prostate Cancer	MEI Pharma Inc.	November 2007	Phase 2
NCT00878800	Completed	Dose Escalation: Solid Tumors\|MTD: Soft Tissue Sarcomas	Valerio Therapeutics\|Spectrum Pharmaceuticals Inc	December 2006	Phase 1\|Phase 2

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):