ETC-159

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ETC-159

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Cat No: 24104

Biochemicals - Small Molecule Inhibitors

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 ca...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

ETC1922159 ETC159 STF-3A PA1 Wnt-1 A1

Product Overview:
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.

Size	1 mg
Shipping	dry ice
CAS Number	1638250-96-0
Molecular Formula	C₁₉H₁₇N₇O₃
SMILES	O=C1N(C)C(C(N(CC(NC2=NN=C(C3=CC=CC=C3)C=C2)=O)C=N4)=C4N1C)=O
Molecular Weight	391,4
Formulation	A crystalline solid
Purity	≥95%
Custom Code	2924.19
UNSPSC code	12352100

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MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.