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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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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].
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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 |
| References | |
| Additional Infomation |
Idronoxil is a substance that is being studied in the treatment of cancer. It belongs to the family of drugs called signal transduction inhibitors.
Idronoxil has been reported in Lespedeza homoloba with data available. Idronoxil is a synthetic flavonoid derivative. Idronoxil activates the mitochondrial caspase system, inhibits X-linked inhibitor of apoptosis (XIAP), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex, thereby preventing DNA replication and resulting in tumor cell death. Drug Indication Intended for the treatment of various forms of cancer. Mechanism of Action The antiproliferative effects of phenoxodiol are associated with inhibition of plasma membrane electron transport in tumour cell lines and primary immune cells. Results from one study (PMID: 17904534) indicate that plasma membrane electron transport (PMET) may be a primary target for phenoxodiol in tumour cells and in activated T cells. Pharmacodynamics Phenoxodiol inhibits proliferation of many cancer cell lines and induces apoptosis by disrupting FLICE-inhibitory protein, FLIP, expression and by caspase-dependent and -independent degradation of the X-linked inhibitor of apoptosis, XIAP. In addition, phenoxodiol sensitizes drug-resistant tumour cells to anticancer drugs including paclitaxel, carboplatin and gemcitabine. |
| 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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