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AZD3514

Catalog No.GC10372

AZD3514 es un inhibidor selectivo del receptor de andrÓgenos (AR) activo por vÍa oral. AZD3514 dependiente e independiente de andrÓgenos inhibe la seÑal AR. AZD351 regula a la baja los niveles de AR nuclear en células de cÁncer de prÓstata LNCaP humanas en ausencia de andrÓgenos con un valor pIC50 de 5,75. AZD3514 se puede utilizar para la investigaciÓn del cÁncer de prÓstata.

Products are for research use only. Not for human use. We do not sell to patients.

AZD3514 Chemical Structure

Cas No.: 1240299-33-5

Tamaño Precio Disponibilidad Cantidad
10mM (in 1mL DMSO)
77,00 $
Disponible
5mg
67,00 $
Disponible
10mg
117,00 $
Disponible
50mg
335,00 $
Disponible
100mg
544,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

AZD3514 is a potent and oral androgen receptor (AR) inhibitor with Ki value of 2.2 μM [1].
AR is a member of the steroid hormone receptor family and functions as a ligand-dependent transcription factor. AR signaling participates in the antiandrogen therapies [2].
In LNCaP and LAPC4 prostate cancer cells, AZD3514 inhibited DHT-driven proliferation of LNCaP cells in a dose-dependent way and inhibited the ligand-driven expression of AR-regulated genes PSA and TMPRSS2. Also, AZD3514 reduced AR protein expression in a dose-dependent way [2].
In male Copenhagen rats with prostate tumors, Oral treatment of AZD3514 (50 mg/kg) once daily inhibited tumor growth by 64%. Also, AZD3514 reduced nuclear AR protein expression. In the Dunning R3327H tumor model, treatment with AZD3514 significantly reduced AR staining in the nucleus of tumor cells, which were caused by reducing the rate of AR synthesis [2].
References:
[1]. Bradbury RH, Acton DG, Broadbent NL, et al. Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer. Bioorg Med Chem Lett, 2013, 23(7): 1945-1948.
[2]. Loddick SA, Ross SJ, Thomason AG, et al. AZD3514: a small molecule that modulates androgen receptor signaling and function in vitro and in vivo. Mol Cancer Ther, 2013, 12(9): 1715-1727.

Chemical Properties

Cas No. 1240299-33-5 SDF
Chemical Name 1-[4-[2-[4-[1-[3-(trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl]phenoxy]ethyl]piperazin-1-yl]ethanone
Canonical SMILES CC(=O)N1CCN(CC1)CCOC2=CC=C(C=C2)C3CCN(CC3)C4=NN5C(=NN=C5C(F)(F)F)CC4
Formula C25H32F3N7O2 M.Wt 519.56
Solubility ≥ 24.45mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 17 reference(s) in Google Scholar.)

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