WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H206481
CAS#: 1638250-96-0
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.
Hodoodo Cat#: H206481
Name: ETC-159
CAS#: 1638250-96-0
Chemical Formula: C19H19N7O3
Exact Mass: 393.15
Molecular Weight: 393.407
Elemental Analysis: C, 58.01; H, 4.87; N, 24.92; O, 12.20
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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: structure was from Bioorg. Med. Chem. Lett. 25 (2015) 5472–5476.
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The following data is based on the product molecular weight 393.41 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 |
| Formulation protocol: | |
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| In vivo protocol: |
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.
