AZD3514 | 99.99%(HPLC) | In Stock | Androgen Receptor inhibitor

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

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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Signaling Pathway

Androgen Receptor Signaling Pathway

Choose Selective Androgen Receptor Inhibitors

Biological Activity

Description

AZD3514 is a potent and oral androgen receptor downregulator with K_i 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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT01351688	Completed	Prostate Cancer	AstraZeneca	August 2011	Phase 1
NCT01162395	Completed	Prostate Cancer	AstraZeneca	August 2010	Phase 1

References
[1] Bradbury RH, et al. Bioorg Med Chem Lett, 2013, 23(7), 1945-1948. [2] Sarah A. Loddick, et al. Cancer Res, 2012, 72(8 Suppl), Abstract nr 3848.

References

Chemical Information & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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