An orally bioavailable inhibitor of Wnt signaling
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CCT251545

Item No. 18761

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-[3-chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]-4-pyridinyl]-2,8-diazaspiro[4.5]decan-1-one
CAS Number
1661839-45-7
Molecular Formula
C23H24ClN5O
Formula Weight
421.9
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 50 mg/ml
λmax
274 nm
SMILES
O=C(NCC1)C1(CC2)CCN2C3=C(C4=CC=C(C5=CN(C)N=C5)C=C4)C=NC=C3Cl
InChi Code
InChI=1S/C23H24ClN5O/c1-28-15-18(12-27-28)16-2-4-17(5-3-16)19-13-25-14-20(24)21(19)29-10-7-23(8-11-29)6-9-26-22(23)30/h2-5,12-15H,6-11H2,1H3,(H,26,30)
InChi Key
LBFYQISQYCGDDW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

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    10 mg

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    Product Description

    CCT251545 is an orally bioavailable inhibitor of Wnt signaling (IC50 = 5 nM).1 It is a potent and selective inhibitor of the human mediator complex-associated protein kinases Cdk8 and Cdk19.2 Through its effects on Cdk8 and Cdk19, CCT251545 alters Wnt pathway-regulated gene expression.2 It reduces tumor growth in COLO 205 human colon cancer xenografts after oral dosing (70 mg/kg bid) and in Wnt-dependent tumors.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mallinger, A., Crumpler, S., Pichowicz, M., et al. Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen. J. Med. Chem. 58(4), 1717-1735 (2015).

    2. Dale, T., Clarke, P.A., Esdar, C., et al. A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. Nat. Chem. Biol. 11(12), 973-980 (2015).