ETC-159
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MedKoo CAT#: 206481

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.


Chemical Structure

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ETC-159
CAS# 1638250-96-0

Theoretical Analysis

MedKoo Cat#: 206481
Name: ETC-159
CAS#: 1638250-96-0
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

Price and Availability

Size Price Availability Quantity
50.0mg USD 250.0 2 weeks
100.0mg USD 450.0 2 weeks
200.0mg USD 850.0 2 weeks
500.0mg USD 1650.0 2 weeks
1.0g USD 2950.0 2 weeks
2.0g USD 4650.0 2 weeks
5.0g USD 6950.0 2 weeks
Bulk inquiry

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

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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

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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.

ETC-159

50.0mg / USD 250.0


Additional Information

structure was from Bioorg. Med. Chem. Lett. 25 (2015) 5472–5476.