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| 10mg |
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| Targets |
Idronoxil targets the caspase system, XIAP, FLIP, topoisomerase II, and plasma membrane electron transport (PMET). It activates the mitochondrial caspase system and inhibits X-linked apoptosis inhibitor protein (XIAP). It disrupts FLICE inhibitor protein (FLIP) expression, sensitizing cancer cells to Fas-mediated apoptosis. It induces cell cycle arrest at the G1/S phase by upregulating p21WAF1 in a p53-independent manner. It inhibits DNA topoisomerase II by stabilizing the cleavable complex. Plasma membrane electron transport (PMET) may be a major target.
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| ln Vitro |
In primary ovarian cancer cells, phenoldoxodiol (Idronoxil) (0–10 μg/mL; 24 hours) decreases cell viability [1]. Phenoxodiol (0-10 μg/mL; 24 hours) causes ovarian cancer cells to undergo apoptosis and regains their susceptibility to Fas-mediated apoptosis [1]. Through the Akt pathway, phenoloxodiol (0–10 μg/mL; 24 hours) causes FLIP downregulation and caspase-8 activation. Apoptosis brought on by phenolphthalein is caspase-dependent and includes the activation of mitochondrial mechanisms. Treatment with phenoxodiol causes XIAP cleavage and downregulation [1]. In prostate cancer cells in the G1/S phase of the cell cycle, phenoloxazodiol (10 and 30 μM; 24 and 48 hours) produces cell cycle arrest [2].
In vitro, Idronoxil activates the mitochondrial caspase system, inhibits XIAP, and disrupts FLIP expression, sensitizing cancer cells to Fas-mediated apoptosis. It induces cell cycle arrest at the G1/S phase by upregulating p21WAF1 in a p53-independent manner. It inhibits DNA topoisomerase II by stabilizing the cleavable complex. The compound's in vitro activity is well-characterized and forms the basis for its use in cancer research. |
| ln Vivo |
In vivo, Idronoxil has demonstrated antitumor activity in preclinical models. The compound has been studied in cancer clinical trials. It induces apoptosis in tumor cells through multiple mechanisms.
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| Enzyme Assay |
Cell-free topoisomerase II assays with Idronoxil are performed using purified enzyme and plasmid DNA. The compound is incubated with topoisomerase II and DNA, and DNA cleavage products are analyzed by gel electrophoresis. Caspase activity is measured using fluorogenic substrates. These cell-free assays are essential for characterizing the potency of Idronoxil as a topoisomerase II inhibitor and caspase activator.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: R182s, R127, Hey, CP70, A2780, R187, R188, R207 and OSE Cell Tested Concentrations: 0, 0.01, 0.1, 1 and 10 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: Significant At a concentration of 10 μg/mL (41.6 μM), a decrease in cell viability was observed in all ovarian cancer cell cultures and did not affect the viability of ovarian surface epithelial (OSE) cells. In CP70 cells, the IC50 is 1.35 μM. Apoptosis analysis[1] Cell Types: CP70 and OSE Cell Tested Concentrations: 10 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: Induced apoptosis and resulted in a twofold increase in caspase-3 activity. No changes in caspase-3 activity were found in normal OSE cells. Western Blot Analysis[1] Cell Types: Ovarian cancer cells Tested Concentrations: 10 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: Induction of caspase-8 activation, characterized by cleavage of procaspase-8 into p43/41 and p28 forms, and downregulation of caspase- 8 expression. The P43 form of FLIPC was present in all primary cultures as w In cellular assays, cancer cell lines are treated with Idronoxil at varying concentrations. Cell viability is assessed using MTT assays. Apoptosis is evaluated by Annexin V staining, caspase activity assays, and Western blot for XIAP and FLIP expression. Cell cycle analysis is performed by flow cytometry. These cellular assays are crucial for understanding the functional consequences of Idronoxil treatment and for validating its activity as an anticancer agent. |
| Animal Protocol |
In vivo efficacy of Idronoxil is evaluated in mouse xenograft models of various cancers. The compound is administered orally or intraperitoneally. Tumor growth inhibition, apoptosis markers, and survival are monitored. Clinical trials have been conducted in cancer patients.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Idronoxil including oral bioavailability, half-life, and tissue distribution have been characterized in preclinical and clinical studies. The compound is available as a research compound.
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| Toxicity/Toxicokinetics |
Toxicological evaluation in preclinical studies and clinical trials has assessed the safety profile of Idronoxil. Adverse effects may include gastrointestinal disturbances. The compound is generally well-tolerated at therapeutic doses.
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| References | |
| Additional Infomation |
Idronoxil is a substance under investigation for cancer treatment. It belongs to the class of signal transduction inhibitors. Idronoxil has been reported to exist in Lespedeza homoloba, and relevant data are available. Idronoxil is a synthetic flavonoid derivative. It activates the mitochondrial caspase system, inhibits X-linked apoptosis inhibitor protein (XIAP), and disrupts the expression of FLICE inhibitor protein (FLIP), thereby leading to tumor cell apoptosis. The drug also inhibits DNA topoisomerase II by stabilizing the DNA topoisomerase II cleavage complex, thereby preventing DNA replication and causing tumor cell death. Drug Indications: Used to treat various cancers. Mechanism of Action: The antiproliferative effect of phenoxydiol is related to its inhibition of plasma membrane electron transport in tumor cell lines and primary immune cells. A study (PMID: 17904534) indicated that plasma membrane electron transport (PMET) may be a major target of phenoxydiol in tumor cells and activated T cells.
Pharmacodynamics Phenoxydiol inhibits the proliferation of various cancer cell lines and induces apoptosis by disrupting the expression of the FLICE inhibitor protein FLIP and degrading the X chromosome-linked apoptosis inhibitor XIAP via caspase-dependent and caspase-independent pathways. Furthermore, phenoxydiol can enhance the sensitivity of drug-resistant tumor cells to anticancer drugs including paclitaxel, carboplatin, and gemcitabine. Idronoxil (Phenoxodiol, CAS 81267-65-4) is an investigational anticancer agent. It is a synthetic genistein analog that activates the mitochondrial caspase system and inhibits XIAP. Clinical trials have been conducted in cancer patients. The compound is also known as phenoxodiol. No FDA approval has been reported. The compound should be stored according to the manufacturer's recommendations, typically at -20°C, to ensure stability. When handling Idronoxil, researchers should follow standard safety protocols for handling chemical reagents, including the use of appropriate personal protective equipment and working in a well-ventilated area. |
| Molecular Formula |
C15H12O3
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| Molecular Weight |
240.25398
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| Exact Mass |
240.078
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| CAS # |
81267-65-4
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| PubChem CID |
219100
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| Appearance |
Off-white to brown solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
463.7±45.0 °C at 760 mmHg
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| Flash Point |
234.3±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.679
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| LogP |
4.35
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
318
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZZUBHVMHNVYXRR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H12O3/c16-13-4-1-10(2-5-13)12-7-11-3-6-14(17)8-15(11)18-9-12/h1-8,16-17H,9H2
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| Chemical Name |
3-(4-hydroxyphenyl)-2H-chromen-7-ol
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| Synonyms |
NV 06 NV06 NV-06
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~416.23 mM)
H2O : ~1 mg/mL (~4.16 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.4162 mL | 2.0812 mL | 4.1623 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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