WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206481
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.
MedKoo Cat#: 206481
Chemical Formula: C19H19N7O3
Exact Mass: 393.15494
Molecular Weight: 393.407
Elemental Analysis: C, 58.01; H, 4.87; N, 24.92; O, 12.20
ETC-159, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.
Synonym: ETC-159; ETC159; ETC 159; ETC-1922159; ETC 1922159; ETC1922159.
IUPAC/Chemical Name: 1,3-dimethyl-7-((6-phenylpyridazin-3-yl)glycyl)-3,4,5,7-tetrahydro-1H-purine-2,6-dione
InChi Key: COEZTQWWLJCBEC-UHFFFAOYSA-N
InChi Code: InChI=1S/C19H19N7O3/c1-24-17-16(18(28)25(2)19(24)29)26(11-21-17)15(27)10-20-14-9-8-13(22-23-14)12-6-4-3-5-7-12/h3-9,11,16-17H,10H2,1-2H3,(H,20,23)
SMILES Code: O=C1C2C(N=CN2C(CNC3=CC=C(C4=CC=CC=C4)N=N3)=O)N(C)C(N1C)=O
The following data is based on the product molecular weight 393.407 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Madan B, Ke Z, Harmston N, Ho SY, Frois AO, Alam J, Jeyaraj DA, Pendharkar V, Ghosh K, Virshup IH, Manoharan V, Ong EH, Sangthongpitag K, Hill J, Petretto E, Keller TH, Lee MA, Matter A, Virshup DM. Wnt addiction of genetically defined cancers reversed by PORCN inhibition. Oncogene. 2015 Aug 10. doi: 10.1038/onc.2015.280. [Epub ahead of print] PubMed PMID: 26257057.
structure was from Bioorg. Med. Chem. Lett. 25 (2015) 5472–5476.