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Product Details

THZ1 | Potent and selective CDK7 inhibitor

THZ1 (1604810-83-4) 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

References/Citations

1) Kwiatkowski et al. (2014), Targeting transcription regulation in cancer with a covalent CDK7 inhibitor; Nature, 511 616
2) Chipumuro et al. (2014), CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription of MYCN-driven cancers; Cell , 159 1126
3) Cayrol et al. (2017), THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors; Nature Commun.,8 14290
4) Rusan et al. (2018), Suppression of Adaptive Responses to Targeted Cancer Therapy by Transcriptional Repression; Cancer Discov., 8 59

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Catalog#  10-4120-0005

$80.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
16048-83-4
Catalog Number:
10-4120
Activity:
Potent and selective CDK7 inhibitor
Chemical Name:
(E)-N-(3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)-4-(4-(dimethylamino)but-2-enamido)benzamide
Molecular Weight:
566.05
Molecular Formula:
C31H28ClN7O2
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
Tan solid
Purity:
97% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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