DC Chemicals · Product datasheet

ETC-159 — Datasheet

CAT. NO. DC8489

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ParameterValue
Chemical NameEtc-159
CAS No.1638250-96-0
SynonymsETC-159;5L854240DQ;BCP20688;BDBM50133866;SB18869;2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(6-phenylpyridazin-3-yl)acetamide;2-(1,3-dimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-7-yl)-N-(6-phenylpyridazin-3-yl)acetamide
FormulaC19H17N7O3
M.Wt391.3834
SMILESO=C1C2=C(N=C([H])N2C([H])([H])C(N([H])C2C([H])=C([H])C(C3C([H])=C([H])C([H])=C([H])C=3[H])=NN=2)=O)N(C([H])([H])[H])C(N1C([H])([H])[H])=O
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

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

In Vitro

ETC-159 blocks the secretion and activity of all Wnts. ETC-159 has robust activity in multiple cancer models driven by high Wnt signaling. ETC-159 is highly efficacious in molecularly defined colorectal cancers (CRCs) with R-spondin translocations[1]

In Vivo

ETC-159 inhibits mouse PORCN with an IC50 of 18.1 nM, whereas the IC50 for Xenopus Porcn is approximately four fold higher (70 nM). ETC-159 is remarkably effective in treating RSPO-translocation bearing colorectal cancer (CRC) patient-derived xenografts. ETC-159 exhibits good oral pharmacokinetics in mice allowing preclinical evaluation via oral administration. After a single oral dose of 5 mg/kg, ETC-159 is rapidly absorbed into the blood with a Tmax of ~0.5 h and oral bioavailability of 100%[1].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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