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ECT-159

Chemical Structure : ECT-159

CAS No.: 1638250-96-0

ECT-159 (ETC-1922159)

Catalog No.: PC-72828Not For Human Use, Lab Use Only.

ECT-159 (ETC-1922159) is a potent, orally available Porcupine (PORCN) inhibitor that blocks the secretion and activity of all Wnts, inhibits β-catenin reporter activity with IC50 of 2.9 nM.

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Biological Activity

ECT-159 (ETC-1922159) is a potent, orally available Porcupine (PORCN) inhibitor that blocks the secretion and activity of all Wnts, inhibits β-catenin reporter activity with IC50 of 2.9 nM.
ECT-159 effectively inhibited the secretion of WNT3A into culture media but did not inhibit β-catenin signaling in STF cells supplemented with Wnt3A-conditioned medium.
ETC-159 is orally bioavailable and effectively inhibits the growth of mouse mammary tumor virus (MMTV)-Wnt1 tumors, inhibits Wnt autocrine signaling and growth of teratocarcinomas, significantly reduces the phosphorylation of both Dvl2 and LRP6, prevents growth of colorectal tumors with RSPO fusions, induces global remodeling of gene expression in colon cancers with RSPO translocations.

Physicochemical Properties

M.Wt 391.391
Formula C19H17N7O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(6-phenylpyridazin-3-yl)acetamide

References

1. B Madan, et al. Oncogene. 2016 Apr 28;35(17):2197-207.

2. Madan B, et al. Bone Res. 2018 May 25;6:17.

3. Zhong Z, et al. Oncogene. 2019 Oct;38(40):6662-6677.

4. Liu Z, et al. J Med Chem. 2021 Apr 22;64(8):4257-4288.

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