Home GPCR & G Protein Adenosine Receptor antagonist Imaradenant (AZD4635) For research use only.

Imaradenant (AZD4635)

Synonyms: HTL1071

Imaradenant (AZD4635, HTL1071) is an oral A2AR antagonist that binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors.

Imaradenant (AZD4635) Chemical Structure

Imaradenant (AZD4635) Chemical Structure

CAS No. 1321514-06-0

Purity & Quality Control

Imaradenant (AZD4635) Related Products

Biological Activity

Description Imaradenant (AZD4635, HTL1071) is an oral A2AR antagonist that binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors.
Targets
A2AR [1]
(Cell-free)
1.7 nM(Ki)
In vitro
In vitro

In CHO cells stably expressing human A2AR, the IC50s of AZD4635 for inhibition of cAMP production are 0.79, 10.0 and 142.9 nM in the presense of 0.1, 1 and 10 μM adenosine, respectively[1].
In Vivo
In vivo

Blockade of A2AR signaling with AZD4635 could reduce tumor burden and enhance antitumor immunity[1].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04495179 Completed
Progressive Metastatic Castrate-Resistant Prostate Cancer
AstraZeneca|Parexel
 August 4 2020 Phase 2
NCT04089553 Completed
Prostate Cancer|Metastatic Castration-Resistant Prostate Cancer (mCRPC)
AstraZeneca
 August 29 2019 Phase 2
NCT03381274 Active not recruiting
Carcinoma Non-Small-Cell Lung
MedImmune LLC
 May 8 2018 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 315.73 Formula

C15H11ClFN5
CAS No. 1321514-06-0 SDF --
Smiles CC1=CC(=CC(=N1)Cl)C2=C(N=C(N=N2)N)C3=CC=C(C=C3)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 63 mg/mL ( (199.53 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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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.
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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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