ETC-159 chemical structure
Chemical structureResearch use only
CAT. NO. DC8489Featured

ETC-159

Pack Sizes & Prices

TotalUS$380
We match the best price and quality on market.
Product overview

Description & Application

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

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.

Product documentation

View online datasheetRequest COA / MSDS

Refer to the certificate supplied with your lot for batch-specific release results.

Handling guide

2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Solution calculator

Related research products

Adavivint chemical structureDC11886

Adavivint

Adavivint is a potent and selective inhibitor of canonical Wnt signaling, with an EC50 of 19.5 nM via a high-throughput TCF/LEF-reporter assay in SW480 colon cancer cells.

View activity & prices
AMBMP chemical structureDC9951

AMBMP

AMBMP(BML-284) is potent selective, and cell-permeable Wnt signaling activator.in vitro: BML-284 induces the β-catenin/TCF-dependent reporter in a dose-dependent manner.

View activity & prices
Foxy-5(Wnt5a peptide mimetic) chemical structureDC23893

Foxy-5(Wnt5a peptide mimetic)

Foxy-5 is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 is a WNT5A agonist and effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic…

View activity & prices
JNJ 38877605 chemical structureDC7177

JNJ 38877605

JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.

View activity & prices
GLPG0187 chemical structureDC10034

GLPG0187

GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.

View activity & prices
Omipalisib chemical structureDC7141

Omipalisib

Omipalisib (GSK2126458) is a highly selective and potent inhibitor of PI3K with Kis of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively.

View activity & prices

Cart

Request quotation