Home Endocrinology & Hormones Androgen Receptor inhibitor AZD3514 For research use only.

AZD3514

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.

AZD3514 Chemical Structure

AZD3514 Chemical Structure

CAS: 1240299-33-5

Purity & Quality Control

Batch: S704001 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] Insoluble] false Purity: 99.99%
99.99

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Biological Activity

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.
Targets
Androgen Receptor [1]
2.2 μM(Ki)
In vitro
In vitro

AZD3514 binds to the AR ligand binding domain and has selectivity for binding to AR over other nuclear hormone receptors. 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. AZD3514 causes a rapid reduction in PSA synthesis in vitro; with a significant decrease in PSA mRNA being evident in LNCaP cells within 2-3 h of compound treatment. AZD3514 inhibits an androgen-induced translocation of AR from the cytoplasm to the nucleus within a comparable time-frame in LNCaP cells and U2OS AR-transfected cells. AZD3514 treatment also reduces AR protein in LNCaP cells maintained in steroid-depleted conditions; an effect which is evident within 6-8 h, and maximal at 18-24 h. 
In Vivo
In vivo

The mode of action of AZD3514 is associated with loss of AR function. Administration of AZD3514 (100 mg/kg/day orally) for 3 days to Copenhagen rats bearing R3327H Dunning prostate tumours, indicates that AZD3514 treatment also reduces tumour AR in vivo. [2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01351688 Completed Prostate Cancer AstraZeneca August 2011 Phase 1
NCT01162395 Completed Prostate Cancer AstraZeneca August 2010 Phase 1

Chemical lnformation & Solubility

Molecular Weight 519.56 Formula

C25H32F3N7O2
CAS No. 1240299-33-5 SDF Download AZD3514 SDF
Smiles CC(=O)N1CCN(CC1)CCOC2=CC=C(C=C2)C3CCN(CC3)C4=NN5C(=NN=C5C(F)(F)F)CC4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (192.47 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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