A potent

ETC-159 – 1 mg

Brand:
Cayman
CAS:
1638250-96-0
Storage:
-20
UN-No:
Non-Hazardous - /

ETC-159 is a potent and orally bioavailable inhibitor of porcupine (PORCN; IC50s = 18.1 and 70 nM for mouse and Xenopus PORCN, respectively).{38876} 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.  

 

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SKU: 24104 - 1 mg Category:

Description

A potent, orally bioavailable inhibitor of PORCN (IC50s = 18.1 and 70 nM for mouse and Xenopus PORCN, respectively); 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; inhibits PA-1 teratocarcinoma colony formation in soft agar (IC50 = 35 nM); 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 (1-10 mg/kg); reduces growth and induces differentiation in colon adenocarcinoma mouse xenograft models that contain RSPO translocations,

Formal name: 1,2,3,6-tetrahydro-1,3-dimethyl-2,6-dioxo-N-(6-phenyl-3-pyridazinyl)-7H-purine-7-acetamide

Synonyms:  ETC-1922159

Molecular weight: 391.4

CAS: 1638250-96-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Signaling|Wnt Signaling||Research Area|Cell Biology|Cell Signaling|Wnt Signaling

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