Introduction：Basic information about CAS 1638250-96-0|ETC-159, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | ETC-159 |
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| CAS Number | 1638250-96-0 | Molecular Weight | 391.383 |
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| Density | 1.5±0.1 g/cm3 | Boiling Point | / |
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| Molecular Formula | C19H17N7O3 | Melting Point | / |
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| MSDS | / | Flash Point | / |
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Names
| Name | 1,2,3,6-Tetrahydro-1,3-dimethyl-2,6-dioxo-N-(6-phenyl-3-pyridazinyl)-7H-purine-7-acetamide |
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| Synonym | More Synonyms |
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ETC-159 BiologicalActivity
| Description | ETC-159 is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM. |
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| Related Catalog | Signaling Pathways >>Stem Cell/Wnt >>WntResearch Areas >>Cancer |
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| Target | IC50: 2.9 nM (β-catenin)[1] |
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| 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] |
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| 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]. |
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| Cell Assay | HEK293 cells stably transfected with STF reporter and pPGK-WNT3A plasmid (STF3A cells) are treated with varying concentrations of compounds. For Wnt secretion, STF3A cells are treated with ETC-159 diluted in 1% fetal bovine serum-containing media[1]. |
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| Animal Admin | Mice: For human xenograft models, patient-derived solid tissue fragments are subcutaneously implanted in BALB/c nude mice. All groups are matched for tumor size with equal variance before treatment. ETC-159 formulated in 50% PEG400 (vol/vol) in water is administered by oral gavage at a dosing volume of 10 μL/g body weight[1]. |
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| References | [1]. Madan B, et al. Wnt addiction of genetically defined cancers reversed by PORCN inhibition. Oncogene. 2015 Aug 10. doi: 10.1038/onc.2015.280. |
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Chemical & Physical Properties
| Density | 1.5±0.1 g/cm3 |
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| Molecular Formula | C19H17N7O3 |
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| Molecular Weight | 391.383 |
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| Exact Mass | 391.139282 |
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| LogP | 1.20 |
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| Index of Refraction | 1.732 |
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| InChIKey | QTRXIFVSTWXRJJ-UHFFFAOYSA-N |
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| SMILES | Cn1c(=O)c2c(ncn2CC(=O)Nc2ccc(-c3ccccc3)nn2)n(C)c1=O |
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| Storage condition | 2-8℃ |
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Synonyms
| 2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(6-phenyl-3-pyridazinyl)acetamide |
| 7H-Purine-7-acetamide, 1,2,3,6-tetrahydro-1,3-dimethyl-2,6-dioxo-N-(6-phenyl-3-pyridazinyl)- |
| ETC-159 |
