A TNKS1 and TNSK2 inhibitor (IC50s = 7 and 9.2 nM

Tankyrase-IN-2 – 1 mg

Brand:
Cayman
CAS:
1588870-36-3
Storage:
-20
UN-No:
Non-Hazardous - /

Tankyrase-IN-2 is an inhibitor of the tankyrases TNKS1 and TNKS2 (IC50s = 7 and 9.2 nM, respectively).{50796} It is selective for TNKS1 and TNKS2 over a panel of 10 additional poly(ADP-ribose) polymerases (PARPs; IC50s = 710->10,000 nM for the human enzymes). Tankyrase-IN-2 increases accumulation of Axin2 and TNKS, indicating inhibition of TNKS-mediated auto-PARsylation, in DLD-1 colorectal cancer cells with EC50 values of 319 and 320 nM, respectively. It also increases tumor Axin2 and TNKS accumulation, as well as decreases tumor levels of active β-catenin, in a DLD-1 mouse xenograft model when administered at doses of 10, 30, and 90 mg/kg.  

 

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SKU: 29808 - 1 mg Category:

Description

A TNKS1 and TNSK2 inhibitor (IC50s = 7 and 9.2 nM, respectively); selective for TNKS1 and TNKS2 over a panel of 10 additional PARP enzymes (IC50s = 710->10,000 nM for the human enzymes); increases accumulation of Axin2 and TNKS in DLD-1 colorectal cancer cells (EC50s = 319 and 320 nM, respectively); increases tumor Akin2 and TNKS accumulation, as well as decreases tumor β-catenin levels, in a DLD-1 mouse xenograft model at 10, 30, and 90 mg/kg

Formal name: 6,8-difluoro-2-[4-(1-hydroxy-1-methylethyl)phenyl]-4(3H)-quinazolinone

Synonyms: 

Molecular weight: 316.3

CAS: 1588870-36-3

Purity: ≥98%

Formulation: A crystalline solid

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