(E/Z)-Droloxifene
Based on 1 Customer Validation
(E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC50 value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity.
For research use only. We do not sell to patients.
- Purity : 98.04%
- CAS No.: 165813-01-4
- Formula: C26H29NO2
- Molecular Weight:387.51
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero | CC50 |
15.82 μM
Compound: Droloxifene
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Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
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10.1101/2020.03.20.999730 |
| Vero | IC50 |
6.6 μM
Compound: Droloxifene
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Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
|
10.1101/2020.03.20.999730 |
Chemical Information
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CAS No. 165813-01-4
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Appearance Solid
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Molecular Weight 387.51
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Formula C26H29NO2
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Color White to off-white
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SMILES
OC1=CC=CC(/C(C2=CC=C(C=C2)OCCN(C)C)=C(CC)/C3=CC=CC=C3)=C1
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Synonyms
(E/Z)-3-Hydroxytamoxifen
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Purity & Documentation
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Data Sheet (269 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Robertson JF. Selective oestrogen receptor modulators/new antioestrogens: a clinical perspective. Cancer Treat Rev. 2004 Dec;30(8):695-706. [Content Brief]
[2]. Kawamura I, et al. The estrogenic and antiestrogenic activities of droloxifene in human breast cancers. Jpn J Pharmacol. 1993 Sep;63(1):27-34. [Content Brief]
[3]. Löser R, et al. Pharmacological activities of droloxifene isomers. Anticancer Res. 1988 Nov-Dec;8(6):1271-4. [Content Brief]
[4]. Hasmann M, et al. Preclinical data for Droloxifene. Cancer Lett. 1994 Sep 15;84(2):101-16. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)