AZD3514

SKU: orb1226692

Description

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.

Key Properties

• CAS Number: 1240299-33-5
• MW: 519.56
• Purity: >98% (HPLC)
• Formula: C??H??F?N?O?
• SMILES: CC(N1CCN(CCOC2=CC=C(C3CCN(C4=NN5C(CC4)=NN=C5C(F)(F)F)CC3)C=C2)CC1)=O
• Target: Androgen Receptor (AR)
• Solubility: DMSO:93 mg/mL (179 mM);Ethanol:93 mg/mL (179 mM);Water:<1 mg/mL

Bioactivity

• In Vivo:
  AZD3514 (10-100 mg/kg; p.o. once daily for 6 days) inhibits AR signaling in rats. AZD3514 (50 mg/kg; p.o. once daily for 30 days) inhibits prostate tumor growth. AZD3514 (50-100 mg/kg; p.o. once daily for 3 days) significantly reduces nuclear AR protein In vivo. Animal model: Intact or castrat 42-and 49-day-old Hans Wistar rats. 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. Dosage: 50 mg/kg. Administration: Oral gavage; 50 mg/kg once daily; for 30 days. Result: Significantly inhibited prostate tumor growth of rats.
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• In Vitro:
  AZD3514 (0-10 μM/L; 7 d) inhibits LNCaP and LAPC4 cells proliferation. AZD3514 (0-10 μM/L; 24 h) inhibits the ligand-driven expression of known AR-regulated genes. AZD3514 (0-30 μM/L; 24 h) reduces AR protein expression in LNCaPs and LAPC4s. AZD3514 (1-10 μM/L; 2 h) reduces AR nuclear translocation in LNCaP cells.: Cell Proliferation Assay 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. 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 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AZD3514 | AZD 3514 | AZD-3514

Quick Database Links

Gene Symbol

Androgen Receptor (AR)