A potent, orally bioavailable inhibitor of PORCN
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ETC-159

Item No. 24104

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,2,3,6-tetrahydro-1,3-dimethyl-2,6-dioxo-N-(6-phenyl-3-pyridazinyl)-7H-purine-7-acetamide
CAS Number
1638250-96-0
Synonyms
  • ETC-1922159
Molecular Formula
C19H17N7O3
Formula Weight
391.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMSO: 33 mg/mlDMSO:PBS (pH 7.2) (1:7): 0.12 mg/ml
λmax
270 nm
SMILES
O=C1N(C)C(C(N(CC(NC2=NN=C(C3=CC=CC=C3)C=C2)=O)C=N4)=C4N1C)=O
InChi Code
InChI=1S/C19H17N7O3/c1-24-17-16(18(28)25(2)19(24)29)26(11-20-17)10-15(27)21-14-9-8-13(22-23-14)12-6-4-3-5-7-12/h3-9,11H,10H2,1-2H3,(H,21,23,27)
InChi Key
QTRXIFVSTWXRJJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Product Description

    ETC-159 is a potent and orally bioavailable inhibitor of porcupine (PORCN; IC50s = 18.1 and 70 nM for mouse and Xenopus PORCN, respectively).1 It inhibits β-catenin reporter activity (IC50 = 2.9 nM) and reduces the interaction of Wnt with its carrier protein WLS via decreased Wnt palmitoleation in STF3A cells, an effect that is reversed by overexpression of recombinant PORCN. ETC-159 inhibits PA-1 teratocarcinoma colony formation in soft agar (IC50 = 35 nM). In vivo, ETC-159 (1-10 mg/kg) reduces tumor growth in a dose-dependent manner in mice carrying a mouse mammary tumor virus LTR-Wnt1 transgene and in A-1 and NCCIT teratocarcinoma mouse xenograft models. It also reduces growth and induces differentiation in colon adenocarcinoma mouse xenograft models that contain R-spondin (RSPO) translocations.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Madan, B., Ke, Z., Harmston, N., et al. Wnt addiction of genetically defined cancers reversed by PORCN inhibition. Oncogene 35(17), 2197-2207 (2016).