AZD3514
Based on 3 publication(s) in Google Scholar
AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer.
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- Purity: 99.65%
- CAS No.: 1240299-33-5
- 화학식: C25H32F3N7O2
- 분자량:519.56
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Orally Active Compound Library
HY-L061
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Transcription Factor-Targeted Library
HY-L090
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Anti-Prostate Cancer Compound Library
HY-L124
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Nuclear Receptor Compound Library
HY-L126
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Heterocyclic Compound Library
HY-L138
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Clinical Compound Library Plus
HY-L026P
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Anti-Cancer Compound Library
HY-L025
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Clinical Compound Library
HY-L026
Publications Citing Use of MedChemExpress (MCE) AZD3514
More
Biological Activity
AZD3514 (0-10 μM/L; 7 d) inhibits LNCaP and LAPC4 cells proliferation[2]. AZD3514 (0-10 μM/L; 24 h) inhibits the ligand-driven expression of known AR-regulated genes[2]. AZD3514 (0-30 μM/L; 24 h) reduces AR protein expression in LNCaPs and LAPC4s[2]. AZD3514 (1-10 μM/L; 2 h) reduces AR nuclear translocation in LNCaP cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP and LAPC4 cell lines
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Concentration:0, 0.1, 0.4, 1.1, 3.3 and 10 μM/L
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Incubation Time:7 days
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Result:Inhibited LAPC4 cells growth and dose-dependently inhibited proliferation of LNCaP cells.
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Cell Line:LNCaP and LAPC4 cell lines
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Concentration:0, 0.4, 1.1, 3.3, 10 and 30 μM/L
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Incubation Time:0-24 hours
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Result:Dose-dependently reduced AR protein expression in LNCaPs, and decreased AR protein in LAPC4 cells with a concentration of 10 μM/L. Reduced the rate of AR synthesis to reduce the concentration of AR protein.
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Cell Line:LNCaP and LAPC4 cell lines
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Concentration:0, 0.4, 1.1, 3.3 and 10 μM/L
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Incubation Time:24 hours
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Result:Inhibited ligand-driven expression of AR-regulated genes PSA and TMPRSS2 in both LNCaP and LAPC4 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Intact or castrat 42- and 49-day-old Hans Wistar rats[2]
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Dosage:10, 50 and 100 mg/kg
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Administration:Oral gavage; 10-100 mg/kg once daily; for 6 days
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Result:Inhibited AR signaling in rats, reduced seminal vesicle weight in intact rats, and inhibited the ability of exogenous testosterone proprionate to cause an increase in seminal vesicle weight in castrated rat.
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Animal Model:Male Copenhagen rats with Dunning R3327H prostate tumors[2]
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Dosage:50 mg/kg
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Administration:Oral gavage; 50 mg/kg once daily; for 30 days
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Result:Significantly inhibited prostate tumor growth of rats.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1240299-33-5
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Appearance Solid
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분자량 519.56
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화학식 C25H32F3N7O2
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Color White to off-white
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SMILES
CC(N1CCN(CCOC2=CC=C(C3CCN(C4=NN5C(CC4)=NN=C5C(F)(F)F)CC3)C=C2)CC1)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Mol Cancer Ther
2016 Jul;15(7):1702-12. PMID: 27196756 -
Biochim Biophys Acta Mol Basis Dis
Methylglyoxal induces endothelial cell apoptosis and coronary microvascular dysfunction through regulating AR-cPLA2 signaling. [Abstract]2024 Oct;1870(7):167437. PMID: 39067539 -
Arch Pharm (Weinheim)
Design, synthesis, and characterization of PROTACs targeting the androgen receptor in prostate and lung cancer models. [Abstract]2022 May;355(5):e2100467. PMID: 35128717
용액&용해도
DMSO : ≥ 100 mg/mL (192.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (4.81 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 (4.81 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.
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.
순도&문서
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Data Sheet (276 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Bradbury RH, et al. Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer. Bioorg Med Chem Lett. 2013 Apr 1;23(7):1945-8. [Content Brief]
[2]. Loddick SA, et al. AZD3514: a small molecule that modulates androgen receptor signaling and function in vitro and in vivo. Mol Cancer Ther. 2013 Sep;12(9):1715-27. [Content Brief]
[3]. Omlin A, et al. AZD3514, an oral selective androgen receptor down-regulator in patients with castration-resistant prostate cancer - results of two parallel first-in-human phase I studies. Invest New Drugs. 2015 Jun;33(3):679-90. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9247 mL | 9.6235 mL | 19.2471 mL | 48.1176 mL |
| 5 mM | 0.3849 mL | 1.9247 mL | 3.8494 mL | 9.6235 mL | |
| 10 mM | 0.1925 mL | 0.9624 mL | 1.9247 mL | 4.8118 mL | |
| 15 mM | 0.1283 mL | 0.6416 mL | 1.2831 mL | 3.2078 mL | |
| 20 mM | 0.0962 mL | 0.4812 mL | 0.9624 mL | 2.4059 mL | |
| 25 mM | 0.0770 mL | 0.3849 mL | 0.7699 mL | 1.9247 mL | |
| 30 mM | 0.0642 mL | 0.3208 mL | 0.6416 mL | 1.6039 mL | |
| 40 mM | 0.0481 mL | 0.2406 mL | 0.4812 mL | 1.2029 mL | |
| 50 mM | 0.0385 mL | 0.1925 mL | 0.3849 mL | 0.9624 mL | |
| 60 mM | 0.0321 mL | 0.1604 mL | 0.3208 mL | 0.8020 mL | |
| 80 mM | 0.0241 mL | 0.1203 mL | 0.2406 mL | 0.6015 mL | |
| 100 mM | 0.0192 mL | 0.0962 mL | 0.1925 mL | 0.4812 mL |
AZD3514 Related Classifications
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