DATASHEET
Formulation
Pale yellow solid
Storage:
-20°C
Product Information:
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 IC50’s 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
Description:
CAS Number: 1604810-83-4<br></br>Chemical Name: (E)-N-(3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)-4-(4-(dimethylamino)but-2-enamido)benzamide<br></br>Molecular weight: 566.05<br></br>Formula: C31H28ClN7O2 <br></br>Solubility: DMSO (>25 mg/ml)<br></br>Physical Properties: Tan solid<br></br>Purity: 97% by HPLC