2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. AZD3514

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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AZD3514 Chemical Structure

AZD3514 Chemical Structure

CAS No. : 1240299-33-5

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10 mM * 1 mL in DMSO
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Based on 3 publication(s) in Google Scholar

AZD3514 Related Antibodies

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Description

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[1][2][3].

In Vitro

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.

AZD3514 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: LNCaP and LAPC4 cell lines
Concentration: 0, 0.1, 0.4, 1.1, 3.3 and 10 μM/L
Incubation Time: 7 days
Result: Inhibited LAPC4 cells growth and dose-dependently inhibited proliferation of LNCaP cells.

Western Blot Analysis[2]

Cell Line: LNCaP and LAPC4 cell lines
Concentration: 0, 0.4, 1.1, 3.3, 10 and 30 μM/L
Incubation Time: 0-24 hours
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.

RT-PCR[2]

Cell Line: LNCaP and LAPC4 cell lines
Concentration: 0, 0.4, 1.1, 3.3 and 10 μM/L
Incubation Time: 24 hours
Result: Inhibited ligand-driven expression of AR-regulated genes PSA and TMPRSS2 in both LNCaP and LAPC4 cells.
In Vivo

AZD3514 (10-100 mg/kg; p.o. once daily for 6 days) inhibits AR signaling in rats[2].
AZD3514 (50 mg/kg; p.o. once daily for 30 days) inhibits prostate tumor growth[2].
AZD3514 (50-100 mg/kg; p.o. once daily for 3 days) significantly reduces nuclear AR protein in vivo[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Intact or castrat 42- and 49-day-old Hans Wistar rats[2]
Dosage: 10, 50 and 100 mg/kg
Administration: Oral gavage; 10-100 mg/kg once daily; for 6 days
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.
Animal Model: Male Copenhagen rats with Dunning R3327H prostate tumors[2]
Dosage: 50 mg/kg
Administration: Oral gavage; 50 mg/kg once daily; for 30 days
Result: Significantly inhibited prostate tumor growth of rats.
Clinical Trial
Molecular Weight

519.56

Formula

C25H32F3N7O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(N1CCN(CCOC2=CC=C(C3CCN(C4=NN5C(CC4)=NN=C5C(F)(F)F)CC3)C=C2)CC1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9247 mL 9.6235 mL 19.2471 mL
5 mM 0.3849 mL 1.9247 mL 3.8494 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.00%

SDS (252 KB)

COA (245 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
References

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
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AZD3514 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZD35141240299-33-5AZD 3514AZD-3514Androgen ReceptororalselectiveAR proteinprostate canceranti tumorLNCaPLAPC4ratanti proliferationInhibitorinhibitorinhibit

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