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ETC-159

CAT: 0013-GTR19160464-06Size: 25 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19160464-06Size:25 mg
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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. (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 (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%.
CAS Number
1638250-96-0
Product Name Alternative
ETC-159 | ETC159 | ETC 159 | ETC-1922159
Purity
>98% (HPLC)
Solubility
DMSO : ≥ 34 mg/m; L86.87 mM
Smiles
O=c1c2c (ncn2CC (=O) Nc2ccc (c3ccccc3) nn2) n (C) c (=O) n1C
Molecular Formula
C19H17N7O3
Molecular Weight
391.38
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
1,3-dimethyl-7- ((6-phenylpyridazin-3-yl) glycyl) -3,4,5,7-tetrahydro-1H-purine-2,6-dione

Chemical Information

Etc-159

Porcupine Inhibitor ETC-159 is an orally bioavailable inhibitor of the membrane-bound O-acyltransferase (MBOAT) porcupine (PORCN), with potential antineoplastic activity. Upon oral administration, ETC-159 binds to and inhibits PORCN in the endoplasmic reticulum (ER), which blocks post-translational palmitoylation of Wnt ligands and inhibits their secretion. This prevents the activation of Wnt ligands, interferes with Wnt-mediated signaling, and inhibits cell growth in Wnt-driven tumors. Porcupine catalyzes the palmitoylation of Wnt ligands, and plays a key role in Wnt ligand secretion. Wnt signaling is dysregulated in a variety of cancers.

CAS Number1638250-96-0
PubChem CID86280523
IUPAC Name2-(1,3-dimethyl-2,6-dioxopurin-7-yl)-N-(6-phenylpyridazin-3-yl)acetamide
Molecular FormulaC19H17N7O3
Molecular Weight391.4
XLogP0.5
Topological Polar Surface Area113
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count6
Rotatable Bond Count4
Heavy Atom Count29
Formal Charge0
Complexity654
SMILES
CN1C2=C(C(=O)N(C1=O)C)N(C=N2)CC(=O)NC3=NN=C(C=C3)C4=CC=CC=C4
InChI
InChI=1S/C19H17N7O3/c1-24-17-16(18(28)25(2)19(24)29)26(11-20-17)10-15(27)21-14-9-8-13(22-23-14)12-6-4-3-5-7-12/h3-9,11H,10H2,1-2H3,(H,21,23,27)
InChIKey
QTRXIFVSTWXRJJ-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Etc-159
CAS: 1638250-96-0
CID: 86280523
Formula: C19H17N7O3
MW: 391.4
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight391.4
XLogP30.5
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count6
Rotatable Bond Count4
Exact Mass391.13928743
Monoisotopic Mass391.13928743
Topological Polar Surface Area113 Ų
Heavy Atom Count29
Formal Charge0
Complexity654
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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Alternative Products

CatalogName
BA9073-100ETC-159

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