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AZD3514
Cat No.
CEI-1231
Description
AZD3514 is a small-molecule downregulator of androgen receptor with Ki value of2.2 μM.
Product Overview
AZD3514 is a potent and oral androgen receptor (AR) inhibitor with Ki value of 2.2 μM. 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. 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. 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.
CAS No.
1240299-33-5
Molecular Weight
519.56
Purity
0.98
Storage
Store at -20°C
Targets
androgen receptor
IC50
2.2 μM (Ki)
Molecular Formula
C25H32F3N7O2
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
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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