research use only
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.
| Related Targets | CXCR1 CXCR2 CXCR4 CXCR3 | Click to Expand |
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In vitro |
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| In vitro | AZD5069 is a slowly reversible antagonist of CXCR2 with effects of time and temperature evident on the pharmacology and binding kinetics[1]. |
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In Vivo |
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| In vivo | In preclinical models, airway neutrophil recruitment in response to inflammatory challenge is abrogated by selective targeting of CXCR2 using AZD5069[2]. |
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| 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 |
References |
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| Molecular Weight | 476.52 | Formula | C18H22F2N4O5S2 |
| CAS No. | 878385-84-3 | SDF | -- |
| Synonyms | N/A | ||
| 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 | ||
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In vitro |
DMSO : 95 mg/mL ( (199.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.) |
Molecular Weight Calculator |
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In vivo Add solvents to the product individually and in order. |
In vivo Formulation Calculator |
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Molarity Calculator
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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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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.
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