Zemirciclib

CAS 2057509-72-3

MF C22H28ClN5O2, 429.9 g/mol

(1S,3R)-3-acetamido-N-[5-chloro-4-(5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)pyridin-2-
yl]cyclohexane-1-carboxamide

(1S,3R)-3-acetamido-N-[5-chloro-4-(5,5-dimethyl-4,6-dihydropyrrolo[1,2-b]pyrazol-3-yl)pyridin-2-yl]cyclohexane-1-carboxamide

(1S,3R)-3-acetamido-N-(5-chloro-4-(5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)pyridin-2-yl)cyclohexanecarboxamide

cyclin-dependent kinase inhibitor, antineoplastic, AZD 4573, UNII-E5XSP3X68B

Zemirciclib is a selective, short-acting inhibitor of the serine/threonine cyclin-dependent kinase 9 (CDK9), the catalytic subunit of the RNA polymerase II (RNA Pol II) elongation factor positive transcription elongation factor b (PTEF-b; PTEFb), with potential antineoplastic activity. Upon intravenous administration, zemirciclib binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II, leading to the inhibition of gene transcription of various anti-apoptotic proteins. This induces cell cycle arrest and apoptosis, and leads to a reduction in tumor cell proliferation. CDK9 regulates elongation of transcription through phosphorylation of RNA polymerase II at serine 2 (p-Ser2-RNAPII). It is upregulated in various tumor cell types and plays a key role in the regulation of Pol II-mediated transcription of anti-apoptotic proteins. Tumor cells are dependent on anti-apoptotic proteins for their survival.

AZD-4573 is a small molecule drug with a maximum clinical trial phase of II and has 1 investigational indication.

• AZD4573 in Novel Combinations With Anti-cancer Agents in Patients With Advanced Blood CancerCTID: NCT04630756Phase: Phase 1/Phase 2Status: CompletedDate: 2025-04-09
• AZD4573 as Monotherapy or in Combinations With Anti-cancer Agents in Patients With r/r PTCL or r/r cHLCTID: NCT05140382Phase: Phase 2Status: CompletedDate: 2024-08-28
• Study to Assess Safety, Tolerability, Pharmacokinetics and Antitumor Activity of AZD4573 in Relapsed/Refractory Haematological MalignanciesCTID: NCT03263637Phase: Phase 1Status: CompletedDate: 2021-10-22

SYN

• Large-Scale Synthesis of AZD4573Publication Name: SynfactsPublication Date: 2022-05-17DOI: 10.1055/s-0041-1738312
• From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer TherapyPublication Name: Journal of Medicinal ChemistryPublication Date: 2022-04-29PMID: 35485642DOI: 10.1021/acs.jmedchem.1c02064
• Lessons Learned from Past Cyclin-Dependent Kinase Drug Discovery EffortsPublication Name: Journal of Medicinal ChemistryPublication Date: 2022-03-02PMID: 35235745DOI: 10.1021/acs.jmedchem.1c02190
• Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological MalignanciesPublication Name: Journal of Medicinal ChemistryPublication Date: 2020-12-11PMID: 33306391DOI: 10.1021/acs.jmedchem.0c01754
• A comprehensive insight on the recent development of Cyclic Dependent Kinase inhibitors as anticancer agentsPublication Name: European Journal of Medicinal ChemistryPublication Date: 2020-10-01PMID: 32707525DOI: 10.1016/j.ejmech.2020.112571
• Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An UpdatePublication Name: Journal of Medicinal ChemistryPublication Date: 2020-08-31PMID: 32866383DOI: 10.1021/acs.jmedchem.0c00744
• AZD4573 Is a Highly Selective CDK9 Inhibitor That Suppresses MCL-1 and Induces Apoptosis in Hematologic Cancer CellsPublication Name: Clinical cancer research : an official journal of the American Association for Cancer ResearchPublication Date: 2020-02-14PMID: 31699827DOI: 10.1158/1078-0432.ccr-19-1853
• A New CDK9 Inhibitor on the Block to Treat Hematologic MalignanciesPublication Name: Clinical cancer research : an official journal of the American Association for Cancer ResearchPublication Date: 2020-02-14PMID: 31843752DOI: 10.1158/1078-0432.ccr-19-3670
• Cyclin dependent kinase (CDK) inhibitors as anticancer drugs: Recent advances (2015–2019)Publication Name: Bioorganic & Medicinal Chemistry LettersPublication Date: 2019-10-15PMID: 31477350DOI: 10.1016/j.bmcl.2019.126637

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2017001354&_cid=P22-MJC84G-87476-1

Example 14: (1S,3R)-3-acetamido-N-(5-chloro-4-(5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)pyridin-2-yl)cyclohexanecarboxamide

PAT

• COMPOUNDS DERIVED FROM POLYCYCLIC AMIDE AS CDK9 INHIBITORS, COMPOSITION AND THEIR USESPublication Number: BR-122019013677-B1Priority Date: 2015-06-29
• Polycyclic amide derivatives as CDK9 inhibitorsPublication Number: KR-102663113-B1Priority Date: 2015-06-29Grant Date: 2024-05-02
• Methods of treating a ras protein-related disease or disorderPublication Number: US-2025049810-A1
• Chemical compoundsPublication Number: TW-I723028-BPriority Date: 2015-06-29Grant Date: 2021-04-01
• Chemical compoundsPublication Number: US-2021171541-A1Priority Date: 2015-06-29
• POLYCYCLIC AMIDA DERIVATIVES AS CDK9 INHIBITORSPublication Number: HR-P20211970-T1Priority Date: 2015-06-29
• Pyridine and pyrimidine derivativesPublication Number: US-11352369-B2Priority Date: 2015-06-29Grant Date: 2022-06-07
• Chemical compoundsPublication Number: US-2022340592-A1Priority Date: 2015-06-29

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/////////Zemirciclib, cyclin-dependent kinase inhibitor, antineoplastic, AZD 4573, UNII-E5XSP3X68B