A TNKS1/2 inhibitor
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

Tankyrase-IN-2

Item No. 29808

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6,8-difluoro-2-[4-(1-hydroxy-1-methylethyl)phenyl]-4(3H)-quinazolinone
CAS Number
1588870-36-3
Molecular Formula
C17H14F2N2O2
Formula Weight
316.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10mg/mLDMSO: 10mg/mLEthanol: 10mg/mLEthanol:PBS (pH 7.2) (1:30): 0.025mg/mL
λmax
241, 291 nm
SMILES
CC(C)(O)C1=CC=C(C2=NC(C(C=C(F)C=C3F)=C3N2)=O)C=C1
InChi Code
InChI=1S/C17H14F2N2O2/c1-17(2,23)10-5-3-9(4-6-10)15-20-14-12(16(22)21-15)7-11(18)8-13(14)19/h3-8,23H,1-2H3,(H,20,21,22)
InChi Key
FHBYLOWAINBPRJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    500 µg

    $124

    Add

    1 mg

    $234

    Add
    Cayman Chemical
    Visit Our Cancer Resource Center
    Find Tools & Resources to Study the Hallmarks of Cancer
    • Cancer cell signaling & regulation
    • Cancer metabolism
    • Tumor microenvironment
    EXPLORE NOW
    Product Description

    Tankyrase-IN-2 is an inhibitor of the tankyrases TNKS1 and TNKS2 (IC50s = 7 and 9.2 nM, respectively).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Buchstaller, H.-P., Anlauf, U., Dorsch, D., et al. Discovery and optimization of 2-arylquinazolin-4-ones into a potent and selective tankyrase inhibitor modulating Wnt pathway activity. J. Med. Chem. 62(17), 7897-7909 (2019).