AZD4573

Catalog No.S8719 Batch:S871903

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Technical Data

Formula

C22H28ClN5O2
Molecular Weight 429.94 CAS No. 2057509-72-3
Solubility (25°C)* In vitro DMSO 86 mg/mL (200.02 mM)
Ethanol 86 mg/mL (200.02 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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)

Cell Assay:

[3]
  • Cell lines

    SLK cells

  • Concentrations

    30 nM

  • Incubation Time

    8 h

  • Method

    Cells were treated with indicated concentrations of drug.
Animal Study:

[4]
  • Animal Models

    Nomo-1 AML xenograft

  • Dosages

    5 mg/kg

  • Administration

    i.p.

Selleck's AZD4573 has been cited by 12 publications

Inherited blood cancer predisposition through altered transcription elongation [ Cell, 2024, 187(3):642-658.e19] PubMed: 38218188
Inherited blood cancer predisposition through altered transcription elongation [ Cell, 2024, 187(3):642-658.e19] PubMed: 38218188
Wogonin protects against bleomycin-induced mouse pulmonary fibrosis via the inhibition of CDK9/p53-mediated cell senescence [ Front Pharmacol, 2024, 15:1407891] PubMed: 39040475
Comprehensive molecular characterization of adenoid cystic carcinoma reveals tumor suppressors as novel drivers and prognostic biomarkers [ J Pathol, 2023, 261(3):256-268] PubMed: 37565350
Nuclear microRNAs release paused Pol II via the DDX21-CDK9 complex [ Cell Rep, 2022, 39(2):110673] PubMed: 35417682
PRC1-independent binding and activity of RYBP on the KSHV genome during de novo infection [ PLoS Pathog, 2022, 18(8):e1010801] PubMed: 36026503
Proteomics and phosphoproteomics of chordoma biopsies reveal alterations in multiple pathways and aberrant kinases activities [ Front Oncol, 2022, 12:941046] PubMed: 36248973
KAP1 is a new non-genetic vulnerability of malignant pleural mesothelioma (MPM) [ NAR Cancer, 2022, 4(3):zcac024] PubMed: 35910692
CDK9 Inhibitor Induces the Apoptosis of B-Cell Acute Lymphocytic Leukemia by Inhibiting c-Myc-Mediated Glycolytic Metabolism [ Front Cell Dev Biol, 2021, 9:641271] PubMed: 33748130
Inhibitors Targeting CDK9 Show High Efficacy against Osimertinib and AMG510 Resistant Lung Adenocarcinoma Cells [ Cancers (Basel), 2021, 13(15)3906] PubMed: 34359807

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.