A TNKS2 inhibitor
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NVP-TNKS656

Item No. 19930

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(cyclopropylmethyl)-4-(4-methoxybenzoyl)-N-[(3,5,7,8-tetrahydro-4-oxo-4H-pyrano[4,3-d]pyrimidin-2-yl)methyl]-1-piperidineacetamide
CAS Number
1419949-20-4
Molecular Formula
C27H34N4O5
Formula Weight
494.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMSO: 33 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.20 mg/ml
λmax
279 nm
SMILES
O=C(N=C(CN(CC1CC1)C(CN2CCC(C(C3=CC=C(OC)C=C3)=O)CC2)=O)N4)C5=C4CCOC5
InChi Code
InChI=1S/C27H34N4O5/c1-35-21-6-4-19(5-7-21)26(33)20-8-11-30(12-9-20)16-25(32)31(14-18-2-3-18)15-24-28-23-10-13-36-17-22(23)27(34)29-24/h4-7,18,20H,2-3,8-17H2,1H3,(H,28,29,34)
InChi Key
DYGBNAYFDZEYBA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $63

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    1 mg

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    5 mg

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    10 mg

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    Product Description

    NVP-TNKS656 is an orally bioavailable inhibitor of tankyrase 2 (TNKS2; IC50 = 6 nM).1 It is selective for TNKS2 over poly(ADP-ribose) polymerase (PARP) 1 and 2 (IC50s = >19 and 32 nM, respectively). NVP-TNKS656 inhibits Wnt ligand-induced signaling with an IC50 value of 3.5 nM in an HEK293 cell reporter assay. In vivo, NVP-TNKS656 (350 mg/kg) reduces Axin 2 mRNA expression, a Wnt/β-catenin target gene, in MMTV-Wnt1 tumor bearing mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shultz, M.D., Cheung, A.K., Kirby, C.A., et al. Identification of NVP-TNKS656: The use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor. J. Med. Chem. 56(16), 6495-6511 (2013).