Estramustine
Based on 1 publication(s) in Google Scholar
Estramustine, an estradiol analog, is an orally active antimicrotubule chemotherapy agent. Estramustine depolymerises microtubules by binding to microtubule associated proteins (MAPs) and/or to tubulin. Estramustine can interfere mitosis, trigger cell death and induce apoptosis, which can be used for the research of cancer like prostate cancer.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.53%
- CAS. Nr.: 2998-57-4
- Formel: C23H31Cl2NO3
- Molecular Weight:440.40
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Apoptosis Compound Library
HY-L003
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Publications Citing Use of MedChemExpress (MCE) Estramustine
More
Biologische Aktivität
Tubulin 1[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
3.4 x 10-6M
Compound: estramustine
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Compound was evaluated for toxicity against HeLa S3 cells
Compound was evaluated for toxicity against HeLa S3 cells
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[PMID: 3735321] |
Estramustine (1 µg/mL, 48 h) suppresses PC3 cell growth[1]. Estramustine (2 µg/mL, 48 h) elevates phosphatidylserine eversion amount on PC3 cells and induces PC3 cell apoptosis through reducing miR-31[1]. Estramustine (0-40 µM, 24-72 h) inhibits cell proliferation and tubulin cytoskeleton in RAW 264.7 cells[2]. Estramustine (10 µM, 24 h) inhibits TGF-β-induced RAW 264.7 cell migration, as well as TGF-β-induced uPA production by inhibiting Smad3 activation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3 cells
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Concentration:1 µg/ mL
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Incubation Time:48 h
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Result:Suppressed PC3 cell growth.
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Cell Line:RAW 264.7 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Disrupted the interphase microtubules.
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Cell Line:18 h of TGF-β treated RAW 264.7 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Inhibited TGF-β-Induced Cell Migration.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human prostate cancer xenograft PAC120[3]
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Dosage:4 or 12 mg/kg, a daily dose for 2 weeks.
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Administration:Intraperitoneal injection
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Result:Inhibited PAC120 tumor growth 53% by day 35.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2998-57-4
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Appearance Solid
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Molecular Weight 440.40
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Formel C23H31Cl2NO3
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Color White to off-white
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SMILES
C[C@@]12[C@](CC[C@@H]2O)([H])[C@@]3([H])[C@@](CC1)([H])C4=CC=C(OC(N(CCCl)CCCl)=O)C=C4CC3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (227.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. C Wei, et al. Estramustine phosphate induces prostate cancer cell line PC3 apoptosis by down-regulating miR-31 levels. Eur Rev Med Pharmacol Sci. 2018 Jan;22(1):40-45. [Content Brief]
[2]. Sonja S Mojsilovic, et al. Estramustine Phosphate Inhibits TGF- β-Induced Mouse Macrophage Migration and Urokinase-Type Plasminogen Activator Production. Anal Cell Pathol (Amst). 2018 Sep 2;2018:3134102. [Content Brief]
[3]. Stephane Oudard, et al. Activity of docetaxel with or without estramustine phosphate versus mitoxantrone in androgen dependent and independent human prostate cancer xenografts. J Urol. 2003 May;169(5):1729-34. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2707 mL | 11.3533 mL | 22.7066 mL | 56.7666 mL |
| 5 mM | 0.4541 mL | 2.2707 mL | 4.5413 mL | 11.3533 mL | |
| 10 mM | 0.2271 mL | 1.1353 mL | 2.2707 mL | 5.6767 mL | |
| 15 mM | 0.1514 mL | 0.7569 mL | 1.5138 mL | 3.7844 mL | |
| 20 mM | 0.1135 mL | 0.5677 mL | 1.1353 mL | 2.8383 mL | |
| 25 mM | 0.0908 mL | 0.4541 mL | 0.9083 mL | 2.2707 mL | |
| 30 mM | 0.0757 mL | 0.3784 mL | 0.7569 mL | 1.8922 mL | |
| 40 mM | 0.0568 mL | 0.2838 mL | 0.5677 mL | 1.4192 mL | |
| 50 mM | 0.0454 mL | 0.2271 mL | 0.4541 mL | 1.1353 mL | |
| 60 mM | 0.0378 mL | 0.1892 mL | 0.3784 mL | 0.9461 mL | |
| 80 mM | 0.0284 mL | 0.1419 mL | 0.2838 mL | 0.7096 mL | |
| 100 mM | 0.0227 mL | 0.1135 mL | 0.2271 mL | 0.5677 mL |
Estramustine Related Classifications
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