AZD4573

Catalog No.S8719

For research use only.

AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases.

AZD4573 Chemical Structure

CAS No. 2057509-72-3

Selleck's AZD4573 has been cited by 5 Publications

Purity & Quality Control

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Biological Activity

Description AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases.
Targets
CDK9 [1]
<0.004 μM
In vitro

Short-term treatment with AZD4573 leads to a rapid dose- and time-dependent decrease in cellular pSer2-RNAPII, resulting in activation of caspase 3 and cell apoptosis in a broad range of haematological cancer cell lines (e.g. caspase activation EC50 0.0137 μM in an acute myeloid leukemia model MV4-11)[1]. In human cancer cell line panel screens, AZD4573 demonstrates the ability to induce rapid caspase activation (6h) and loss of viability (24h) across a diverse set of hematological cancers (median caspase EC50 = 30 nM, GI50 = 11 nM) but with minimal effect on solid tumors (median EC50 & GI50 >30 μM)[2].

In vivo

AZD4573 exhibits a short half-life in multiple preclinical species (less than one hour in rat, dog and monkey) and good solubility for intravenous administration[1].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 429.94
Formula

C22H28ClN5O2

CAS No. 2057509-72-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=O)NC1CCCC(C1)C(=O)NC2=NC=C(C(=C2)C3=C4CC(CN4N=C3)(C)C)Cl

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05140382 Recruiting Drug: AZD4573 Relapsed/Refractory Peripheral T-cell Lymphoma|Relapsed/Refractory Classical Hodgkins Lymphoma AstraZeneca December 15 2021 Phase 2
NCT04630756 Recruiting Drug: AZD4573|Drug: Acalabrutinib Advanced Haematological Malignancies AstraZeneca|Parexel February 17 2021 Phase 1|Phase 2
NCT03263637 Completed Drug: AZD4573 Relapsed or Refractory Haematological Malignancies Including|Acute Myeloid Leukemia|Acute Lymphocytic Leukemia|Chronic Lymphocytic Leukemia|High Risk Myelodysplastic Syndrome|Chronic Myelomonocytic Leukemia|Richter''s Syndrome|B-cell Non-Hodgkin Lymphoma|T-cell Non-Hodgkin Lymphoma|Small Lymphocytic Lymphoma|Multiple Myeloma AstraZeneca October 24 2017 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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