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5mg |
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10mg |
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Other Sizes |
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(E)-4-Hydroxytamoxifen (Afimoxifene) is the less active isomer of 4-Hydroxytamoxifen. 4-Hydroxytamoxifen is the active metabolite of tamoxifen which is an anticancer drug and a SERM/selective estrogen receptor modulator.
Targets |
Estrogen Receptor/ERR
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ln Vitro |
Afimoxifene is a tamoxifen metabolite with both estrogenic and anti-estrogenic effects. Afimoxifene has a higher affinity for the estrogen receptor than tamoxifen, and functions as an antagonist in breast cancer cells.
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Additional Infomation |
For the potential treatment of menstrual-cycle related mastalgia, fibrocystic breast disease, breast disease, gynecomastia and Keloid scarring.
4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol is a stilbenoid. ChEBI Afimoxifene (4-Hydroxytamoxifen, trade name TamoGel) is a new estrogen inhibitor under investigation for a variety of estrogen-dependent conditions, including cyclic breast pain and gynecomastia. TamoGel is formulated using Enhanced Hydroalcoholic Gel (EHG) Technology. This technology enables percutaneous delivery of drugs that cannot be delivered orally. It is being developed by Ascent Therapeutics. |
Molecular Formula |
C26H29NO2
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Molecular Weight |
387.51396
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Exact Mass |
387.22
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Elemental Analysis |
C, 80.59; H, 7.54; N, 3.61; O, 8.26
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CAS # |
174592-47-3
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Related CAS # |
4-Hydroxytamoxifen;68047-06-3;(E/Z)-4-Hydroxytamoxifen;68392-35-8; 174592-47-3 (E-isomer)
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PubChem CID |
5352135
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Appearance |
White to off-white solid powder
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Density |
1.092g/cm3
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Boiling Point |
514.4ºC at 760 mmHg
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Flash Point |
264.9ºC
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Vapour Pressure |
3.35E-11mmHg at 25°C
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Index of Refraction |
1.596
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LogP |
5.7
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tPSA |
32.7
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SMILES |
CN(C)CCOC1C=CC(/C(/C2C=CC(O)=CC=2)=C(\C2C=CC=CC=2)/CC)=CC=1
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InChi Key |
TXUZVZSFRXZGTL-OCEACIFDSA-N
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InChi Code |
InChI=1S/C26H29NO2/c1-4-25(20-8-6-5-7-9-20)26(21-10-14-23(28)15-11-21)22-12-16-24(17-13-22)29-19-18-27(2)3/h5-17,28H,4,18-19H2,1-3H3/b26-25+
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Chemical Name |
4-[(E)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol
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Synonyms |
Afimoxifene; Afimoxifene, E-isomer; 68392-35-8; E-4-Hydroxytamoxifen; AKE3PH0IML; CHEMBL279301; (E)-4-Hydroxytamoxifen; cis-4-Hydroxytamoxifen; 4-((1E)-1-(4-(2-(Dimethylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol
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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 : ~12.5 mg/mL (~32.26 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.23 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 12.5 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: ≥ 1.25 mg/mL (3.23 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 12.5 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: ≥ 1.25 mg/mL (3.23 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 | 2.5806 mL | 12.9029 mL | 25.8058 mL | |
5 mM | 0.5161 mL | 2.5806 mL | 5.1612 mL | |
10 mM | 0.2581 mL | 1.2903 mL | 2.5806 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.