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Synonyms: AZD-4573 | compound 24 [PMID: 33306391]
Compound class: Synthetic organic
Comment: AZD4573 is a potent inhibitor of cyclin dependent kinase 9 (CDK9), that was designed for potential to treat haematological malignancies [1-3]. Inhibition of CDK9 disrupts the expression of cancer-promoting genes such as MCL-1, and induces apoptosis.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Alcon C, Manzano-Muñoz A, Montero J. (2020)
A New CDK9 Inhibitor on the Block to Treat Hematologic Malignancies.
Clin Cancer Res, 26 (4): 761-763. [PMID:31843752]
2. Barlaam B, Casella R, Cidado J, Cook C, De Savi C, Dishington A, Donald CS, Drew L, Ferguson AD, Ferguson D et al.. (2020)
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.
J Med Chem, 63 (24): 15564-15590. [PMID:33306391]
3. Cidado J, Boiko S, Proia T, Ferguson D, Criscione SW, San Martin M, Pop-Damkov P, Su N, Roamio Franklin VN, Sekhar Reddy Chilamakuri C et al.. (2020)
AZD4573 Is a Highly Selective CDK9 Inhibitor That Suppresses MCL-1 and Induces Apoptosis in Hematologic Cancer Cells.
Clin Cancer Res, 26 (4): 922-934. [PMID:31699827]