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| Cas No.: | 1638250-96-0 |
| Chemical Name: | Etc-159 |
| Synonyms: | ETC-159;5L854240DQ;BCP20688;BDBM50133866;SB18869;2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(6-phenylpyridazin-3-yl)acetamide;2-(1,3-dimethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-7-yl)-N-(6-phenylpyridazin-3-yl)acetamide |
| SMILES: | O=C1C2=C(N=C([H])N2C([H])([H])C(N([H])C2C([H])=C([H])C(C3C([H])=C([H])C([H])=C([H])C=3[H])=NN=2)=O)N(C([H])([H])[H])C(N1C([H])([H])[H])=O |
| Formula: | C19H17N7O3 |
| M.Wt: | 391.3834 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | ETC-159 is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM. |
| 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]. |
| 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] |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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