Home Immunology & Inflammation CXCR inhibitor AZD5069 For research use only.

AZD5069

AZD5069 is a novel antagonist of CXCR2, which is shown to inhibit binding of CXCL8 to CXCR2 with a pIC50 value of 8.8 and inhibit CXCL8 binding to CXCR1 with pIC50 values of 6.5.

AZD5069 Chemical Structure

AZD5069 Chemical Structure

CAS No. 878385-84-3

Purity & Quality Control

AZD5069 Related Products

Signaling Pathway

CXCR Signaling Pathways

CXCR Signaling Pathway

Biological Activity

Description AZD5069 is a novel antagonist of CXCR2, which is shown to inhibit binding of CXCL8 to CXCR2 with a pIC50 value of 8.8 and inhibit CXCL8 binding to CXCR1 with pIC50 values of 6.5.
Targets
CXCR2 [1]
In vitro
In vitro

AZD5069 is a slowly reversible antagonist of CXCR2 with effects of time and temperature evident on the pharmacology and binding kinetics[1].
In Vivo
In vivo

In preclinical models, airway neutrophil recruitment in response to inflammatory challenge is abrogated by selective targeting of CXCR2 using AZD5069[2].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03177187 Terminated
Metastatic Castration Resistant Prostate Cancer
Institute of Cancer Research United Kingdom|Astellas Pharma Inc|AstraZeneca|Prostate Cancer UK
 November 13 2017 Phase 1|Phase 2
NCT01962935 Completed
Chronic Obstructive Pulmonary Disease (COPD).
AstraZeneca
 November 2013 Phase 1
NCT01735240 Completed
Asthma|Pharmacokinetics|Cmax|Tmax|λz|AUC|Ketoconazole|Metabolite
AstraZeneca
 December 2012 Phase 1

Chemical Information & Solubility

Molecular Weight 476.52 Formula

C18H22F2N4O5S2
CAS No. 878385-84-3 SDF --
Smiles CC(C(CO)O)OC1=NC(=NC(=C1)NS(=O)(=O)N2CCC2)SCC3=C(C(=CC=C3)F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 95 mg/mL ( (199.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 19 mg/mL

Water : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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