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  3. AZD3514

AZD3514 

Cat. No.: HY-16079 Purity: 98.77%
Handling Instructions

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.

For research use only. We do not sell to patients.

AZD3514 Chemical Structure

AZD3514 Chemical Structure

CAS No. : 1240299-33-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
50 mg USD 480 In-stock
Estimated Time of Arrival: December 31
100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression. IC50 Value: 2.2 uM (Ki) Target: androgen receptor AZD3514 binds to the AR ligand binding domain and has selectivity for binding to AR over other nuclear hormone receptors [1]. in vitro: AZD3514 inhibits cell growth in prostate cancer cells expressing wild-type (VCaP) and mutated (T877A) AR (LNCaP), but is inactive in AR-negative prostate cancer cells, indicating a dependency on AR for efficacy [2]. in vivo: We assessed activity initially in the Hershberger castrated rat assay in which oral dosing of AZD3514 (100mg/kg once-daily for 7 days) significantly inhibited testosterone-induced growth of sexual accessory organs [2]. Clinical trial: Open-label Prostate Cancer Study. Phase 1

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (192.47 mM)

*"≥" 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
10 mM 0.1925 mL 0.9624 mL 1.9247 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

  • 3.

    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

*All of the co-solvents are provided by MCE.
References
Molecular Weight

519.56

Formula

C₂₅H₃₂F₃N₇O₂

CAS No.

1240299-33-5

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

Purity: 98.77%

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Product Name:
AZD3514
Cat. No.:
HY-16079
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AZD3514

Cat. No.: HY-16079