ETC-159 ( ETC-159; ETC159; ETC 159; ETC-1922159 )

Catalog No. M17355 CAS No. 1638250-96-0

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Product Name

ETC-159
Note

Research use only, not for human use.
Brief Description

ETC-159 is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
Description

ETC-159, also known as ETC-1922159, is a potent, selective and orally available PORCN inhibitor. ETC-159 blocks the secretion and activity of all Wnts. ETC-159 is remarkably effective in treating RSPO-translocation bearing colorectal cancer (CRC) patient-derived xenografts. Inhibition of Wnt signaling by PORCN inhibition holds promise as differentiation therapy in genetically defined human cancers. Enhanced sensitivity to Wnts is an emerging hallmark of a subset of cancers, defined in part by mutations regulating the abundance of their receptors.
Synonyms

ETC-159; ETC159; ETC 159; ETC-1922159
Pathway

Others
Target

Other Targets
Recptor

β-catenin
Research Area

Cancer
Indication

——

CAS Number

1638250-96-0
Formula Weight

391.38
Molecular Formula

C19H17N7O3
Purity

97%
Solubility

DMSO : ≥ 34 mg/m; L86.87 mM
SMILES

O=c1c2c(ncn2CC(=O)Nc2ccc(c3ccccc3)nn2)n(C)c(=O)n1C
Chemical Name

1,3-dimethyl-7-((6-phenylpyridazin-3-yl)glycyl)-3,4,5,7-tetrahydro-1H-purine-2,6-dione

1. Madan B, et al. Wnt addiction of genetically defined cancers reversed by PORCN inhibition. Oncogene. 2015 Aug 10. doi: 10.1038/onc.2015.280.

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