| CAS NO: | 1638250-96-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| Molecular Weight (MW) | 391.38 |
|---|---|
| Formula | C19H17N7O3 |
| CAS No. | 1638250-96-0 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: ≥ 34 mg/mL |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| SMILES | O=C1C2C(N=CN2C(CNC3=CC=C(C4=CC=CC=C4)N=N3)=O)N(C)C(N1C)=O |
| Synonyms | ETC-1922159; ETC 1922159; ETC1922159; ETC-159; ETC159; ETC 159 |
| In Vitro | In vitro activity: ETC-159 (also known as ETC-192215) is a novel, potent and orally bioavailable PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM and 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. Kinase Assay: 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). 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 |
|---|---|
| In Vivo | ETC-159 is remarkably effective in treating RSPO-translocation bearing colorectal cancer (CRC) patient-derived xenografts. 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% |
| Animal model | Mice bearing colorectal cancer (CRC) patient-derived xenografts |
| Formulation & Dosage | Formulated in 50% PEG400 (vol/vol) in water |
| References | Oncogene. 2016 Apr 28;35(17):2197-207. |
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