THZ1, CDK7 inhibitor (TBI4120)
$144.00 – $585.00
CDK7 inhibitor
SKU | Stock | SIZE (mg) | Price | Quantity | ||
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TBI4120-5MG | Yes | 5 MG | $144.00 | |||
TBI4120-25MG | Yes | 25 MG | $585.00 |
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Description
Product Details
Formal Name: (E)-N-(3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)-4-(4-(dimethylamino)but-2-enamido)benzamide
Molecular Formula: C31H28ClN7O2
Formula Weight: 566.05
CAS Number: 1604810-83-4
Purity: >97%
Formulation: powder
Solubility: Soluble in DMSO (up to at least 25 mg/ml)
Storage: -20°C
Stability: ≥ 1 year.
Applications
CDK7 inhibitor
Functions
THZ1 is an irreversible, covalent inhibitor (dual ATP-site and allosteric covalent binding) of CDK7 (IC50 = 15.6nM @ 20min and 3.2nM @ 180 min). 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. 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. 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.
Application Procedures
First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.
Additional information
SIZE (mg) | 25 MG, 5 MG |
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