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AZD5069 CXCR2 Antagonist

Cat.No.S6645

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.
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Quality Control

Batch: Purity: 99.66%
99.66

Solubility

In vitro
Batch:

DMSO : 95 mg/mL (199.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight
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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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%
% Tween 80
% ddH2O
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Calculation results:

Working concentration: mg/ml;

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.

Chemical Information, Storage & Stability

Molecular Weight 476.52 Formula

C18H22F2N4O5S2

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 878385-84-3 -- Storage of Stock Solutions

Synonyms N/A SMILES CC(C(CO)O)OC1=NC(=NC(=C1)NS(=O)(=O)N2CCC2)SCC3=C(C(=CC=C3)F)F

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
CXCR2
In vitro

AZD5069 is a slowly reversible antagonist of CXCR2 with effects of time and temperature evident on the pharmacology and binding kinetics.

In vivo

In preclinical models, airway neutrophil recruitment in response to inflammatory challenge is abrogated by selective targeting of CXCR2 using AZD5069.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-09-26)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03177187 TERMINATED
Metastatic Castration Resistant Prostate Cancer
Institute of Cancer Research, United Kingdom
2017-11-13 PHASE1; PHASE2
NCT02499328 COMPLETED
Advanced Solid Tumors & Metastatic Squamous Cell Carcinoma of the Head and Neck
AstraZeneca
2015-08-06 PHASE1; PHASE2
NCT02583477 COMPLETED
Metastatic Pancreatic Ductal Adenocarcinoma
AstraZeneca
2016-03-25 PHASE1; PHASE2
NCT03177187 Terminated
Metastatic Castration Resistant Prostate Cancer
Institute of Cancer Research United Kingdom|Astellas Pharma Inc|AstraZeneca|Prostate Cancer UK
2017-11-13 Phase 1|Phase 2
NCT01704495 COMPLETED
Asthma
AstraZeneca
2012-11 PHASE2
NCT01890148 COMPLETED
Asthma
AstraZeneca
2014-03 PHASE1

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