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AZD5069 CXCR2 Antagonist

Name: AZD5069
Brand: Selleck Chemicals
SKU: S6645
Availability: InStock
Rating: 5 (3 reviews)

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.

Chemical Structure

Molecular Weight: 476.52

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Quality Control

Batch: Purity: 99.66%

99.66

Related Targets	PD-1/PD-L1 STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor
Other CXCR Inhibitors	SB 225002 WZ811 Reparixin (Repertaxin) LIT-927 Navarixin (SCH-527123) UNBS5162 LY2510924 AMD3465 hexahydrobromide AMG 487 SX-682

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 65%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	8.000mg/ml (16.79mM)	Taking the 1 mL working solution as an example, add 50 μL of 160 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; then continue to add 650 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C(CO)O)OC1=NC(=NC(=C1)NS(=O)(=O)N2CCC2)SCC3=C(C(=CC=C3)F)F

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	[1] https://pubmed.ncbi.nlm.nih.gov/25736418/ [2] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5286957/ [3] https://pubmed.ncbi.nlm.nih.gov/35831885/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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