A TNKS2 inhibitor
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CAY10753

Item No. 30277

Technical Information
Formal Name
2,2'-((piperazine-1,4-diylbis(ethane-2,1-diyl))bis(sulfanediyl))bis(quinazolin-4(3H)-one)
Molecular Formula
C24H26N6O2S2
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMSO: slightly solubleMethanol: slightly soluble
λmax
230, 273 nm
SMILES
O=C1NC(SCCN2CCN(CCSC(N3)=NC4=C(C=CC=C4)C3=O)CC2)=NC5=C1C=CC=C5
InChi Code
InChI=1S/C24H26N6O2S2/c31-21-17-5-1-3-7-19(17)25-23(27-21)33-15-13-29-9-11-30(12-10-29)14-16-34-24-26-20-8-4-2-6-18(20)22(32)28-24/h1-8H,9-16H2,(H,25,27,31)(H,26,28,32)
InChi Key
RHCZTJJJLXGIDT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    CAY10753 is an inhibitor of tankyrase 2 (TNKS2; IC50 = 0.3 nM).1 It is selective for TNKS2 over TNKS1 (IC50 = 6.1 nM), as well as poly(ADP-ribose) polymerase 1 (PARP1) and PARP2 (IC50s = 89.6 and 37.8 nM, respectively). CAY10753 inhibits proliferation of DLD-1 colorectal cancer cells when used at a concentration of 1 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tomassi, S., Pfahler, J., Mautone, N., et alFrom PARP1 to TNKS2 inhibition: A structure-based approach. Med. Chem. Lett. (2020).