THZ1, CAS [[1604810-83-4]]

Produktübersicht

• Artikelname: THZ1, CAS [[1604810-83-4]]
• Artikelnummer: FBM-10-4120
• Hersteller Artikelnummer: 10-4120
• Alternativnummer: FBM-10-4120-5MG, FBM-10-4120-25MG
• Hersteller: Focus Biomolecules
• Kategorie: Biochemikalien
• Alternative Synonym: Chemical Name: (E)-N-(3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)-4-(4-(dimethylamino)but-2-enamido)benzamide

Produktbeschreibung

CDK7 inhibitor

Produkteigenschaften

• Molekulargewicht: 566.05
• Reinheit: 97% by HPLC
• Formulierung: Tan solid
• CAS Nummer: [1604810-83-4]
• Formel: C31H28ClN7O2

Anwendungsbeschreibung

• Anwendungsbeschreibung: THZ1 is an irreversible, covalent inhibitor (dual ATP-site and allosteric covalent binding) of CDK7 (IC50 = 15.6nM 20min and 3.2nM 180 min).1 It displayed broad based antiproliferative activity with IC50s of less than 200nM against 53% of the 1000 cancer cell lines it was tested against. THZ1 disrupts transcription of several proteins including RUNX1, TAL1, and GATA3. It suppresses oncogenic transcription of MYCN-driven cancers.2 THZ1 decreases STAT3 chromatin binding and expression of target genes such as MYC, PIM1, and others in peripheral T-Cell lymphoma cells with the Y640F STAT3 mutation.3 Addition of THZ1 to targeted cancer therapy increases cell death and hinders the development of drug-resistant cell populations in cellular and in vitro cancer models.4