ETC-159

ETC-159 is a potent and orally bioavailable inhibitor of porcupine (PORCN, IC50s = 18.1 and 70 nM for mouse and Xenopus PORCN, respectively). It inhibits beta-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.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: DMF: 33 mg/ml, DMSO: 33 mg/ml, DMSO:PBS (pH 7.2) (1:7): 0.12 mg/ml. lambdamax: 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.