A TNKS1/2 inhibitor
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AZ 6102

Item No. 19898

Technical Information
Formal Name
rel-2-[4-[6-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-4-methyl-3-pyridinyl]phenyl]-3,7-dihydro-7-methyl-4H-pyrrolo[2,3-d]pyrimidin-4-one
CAS Number
1645286-75-4
Molecular Formula
C25H28N6O
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 15 mg/mlDMF:PBS(pH7.2) (1:2): 0.3 mg/mlDMSO: 10 mg/ml
λmax
327 nm
SMILES
C[C@H]1CN(C2=NC=C(C3=CC=C(C4=NC(C(C=CN5C)=C5N4)=O)C=C3)C(C)=C2)C[C@@H](C)N1
InChi Code
InChI=1S/C25H28N6O/c1-15-11-22(31-13-16(2)27-17(3)14-31)26-12-21(15)18-5-7-19(8-6-18)23-28-24-20(25(32)29-23)9-10-30(24)4/h5-12,16-17,27H,13-14H2,1-4H3,(H,28,29,32)/t16-,17+
InChi Key
WCPTUQOMNJBIET-CALCHBBNSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    AZ 6102 is an inhibitor of tankyrases (TNKS) 1 and 2 with IC50 values of 3 and 1 nM, respectively.1 It demonstrates 100-fold selectivity for TNKS1/2 over PARP1, PARP2, and PARP6 (IC50s = 2, 0.5, and >3 µM, respectively).1 By inhibiting TNKS1/2, AZ6120 has been shown to inhibit Wnt signaling in DLD-1 cells with an IC50 value of 5 nM.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Johannes, J.W., Almeida, L., Barlaam, B., et alPyrimidinone nicotinamide mimetics as selective tankyrase and Wnt pathways inhibitors suitable for in vivo pharmacology. ACS Med. Chem. Lett. 6, 254-259 (2015).