| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Droloxifene targets the estrogen receptor (ER). It binds to the ER with high affinity and acts as an antagonist in breast tissue, inhibiting estrogen-dependent tumor growth. Its affinity for the ER is higher than that of tamoxifen.
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| ln Vitro |
Droloxifene (10 nM; 16-18 hours) induces apoptosis in MCF-7 cells[1].
In vitro, droloxifene inhibits the growth of estrogen receptor-positive breast cancer cell lines, such as MCF-7. It is more potent than tamoxifen in some assays. Its antiestrogenic activity is demonstrated by its ability to inhibit estradiol-stimulated cell proliferation. |
| ln Vivo |
Droloxifene (5-20 mg/kg; p.o.; daily for 4 weeks) enhances the BMD of DFM at 10 mg/kg and totally stops the BMC and BMD of DFM from declining when ovariectomized (OVX) is administered at 20 mg/kg/day[3].
In vivo, droloxifene has shown antitumor activity in animal models of breast cancer. It has been evaluated in clinical trials for the treatment of advanced breast cancer. Its efficacy and tolerability profile are similar to those of tamoxifen. |
| Enzyme Assay |
In vitro receptor binding assays for droloxifene are performed using estrogen receptor preparations. Radiolabeled estradiol is used as a tracer in competition binding experiments. The compound's ability to displace the radioligand is measured to calculate its relative binding affinity (RBA).
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| Cell Assay |
For in vitro cellular assays, ER-positive breast cancer cell lines (e.g., MCF-7) are used. Cells are cultured in estrogen-depleted medium and treated with various concentrations of droloxifene, with or without estradiol. Cell proliferation is measured using MTT or BrdU incorporation assays.
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| Animal Protocol |
5-month-old sham-operate rats[3]
5, 10, 20 mg/kg Oral; daily for 4 weeks In vivo animal studies for droloxifene involve xenograft models of ER-positive breast cancer in immunodeficient mice. The compound is administered orally. Tumor growth is monitored over time. Its effects on uterine weight and other estrogen-sensitive parameters are also assessed. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Known human metabolites of 3-hydroxytamoxifen include N-demethyldoloxifen and (2S,3S,4S,5R)-6-[3-[(E)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenoxy]-3,4,5-trihydroxyoxacyclohexane-2-carboxylic acid. 3-Hydroxytamoxifen is a known human metabolite of tamoxifen. Droloxifene has a molecular weight of 387.51 g/mol and a molecular formula of C26H29NO2. It is a solid. It is typically stored at -20°C and is soluble in DMSO. |
| Toxicity/Toxicokinetics |
Droloxifene is generally well-tolerated. Side effects are similar to those of tamoxifen and include hot flashes, nausea, and vaginal discharge. As a tamoxifen metabolite, its safety profile is well-characterized from clinical use of the parent drug.
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| References |
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| Additional Infomation |
Droloxifene is a stilbene compound. A derivative of the triphenylbenzene drug tamoxifen, Droloxifene is a novel selective estrogen receptor modulator (SERM). Droloxifene exhibits faster pharmacokinetics, reaching peak concentration and being eliminated much faster than tamoxifen. It has a higher affinity for estrogen receptors, a higher anti-estrogenic to estrogen ratio, stronger inhibitory effects on cell growth and division in estrogen receptor-positive cell lines, and lower toxicity, properties that theoretically give it an advantage over tamoxifen in the treatment of human breast cancer. Short-term toxicity is generally mild, similar to other anti-estrogenic drugs. Droloxifene appears to be active and tolerable. It may play a special role in cases requiring rapid pharmacokinetics or a higher anti-estrogenic to estrogen ratio. Droloxifene may be a potentially effective treatment for postmenopausal osteoporosis because it prevents bone loss due to estrogen deficiency without causing uterine enlargement. Droloxifene may affect bone and breast tissue because it induces apoptosis. Droloxifene exhibits anti-implantation activity in rats, and this effect does not appear to be entirely due to its anti-estrogenic activity. Droloxifene is a phenolic analogue of tamoxifen, a nonsteroidal selective estrogen receptor modulator (SERM). Droloxifene competitively inhibits the binding of estradiol to estrogen receptors, thereby preventing the receptors from binding to estrogen-responsive elements on DNA. The result is reduced DNA synthesis and a decreased cellular response to estrogen. (National Cancer Institute)
Droloxifene (3-Hydroxytamoxifen) is a potent, orally active antiestrogen and an active metabolite of tamoxifen. It has been studied for breast cancer treatment. |
| Molecular Formula |
C26H29NO2
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|---|---|
| Molecular Weight |
387.51396
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| Exact Mass |
579.247
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| Elemental Analysis |
C, 80.59; H, 7.54; N, 3.61; O, 8.26
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| CAS # |
82413-20-5
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| Related CAS # |
97752-20-0 (citrate);82413-20-5;
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| PubChem CID |
3033767
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| Appearance |
White to off-white solid powder
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| Density |
1.092 g/cm3
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| Boiling Point |
526.6ºC at 760 mmHg
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| Melting Point |
127-129ºC
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| Index of Refraction |
1.596
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| LogP |
4.453
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
29
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| Complexity |
501
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(/C1C=CC=C(O)C=1)(\C1C=CC(OCCN(C)C)=CC=1)=C(\C1C=CC=CC=1)/CC
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| InChi Key |
ZQZFYGIXNQKOAV-OCEACIFDSA-N
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| InChi Code |
InChI=1S/C26H29NO2/c1-4-25(20-9-6-5-7-10-20)26(22-11-8-12-23(28)19-22)21-13-15-24(16-14-21)29-18-17-27(2)3/h5-16,19,28H,4,17-18H2,1-3H3/b26-25+
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| Chemical Name |
3-[(E)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol
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| Synonyms |
Droloxifene; K 060E; K060E; K-060E; K 21060E; K 21060E
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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: ~50 mg/mL (~129.0 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (12.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| 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.
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