ETC-159
产品编号: DC8489
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应用领域
ETC-159是有效的，具有口服活性的 PORCN 抑制剂。抑制β-catenin报告基因活性的 IC50 值为2.9 nM。
| Cas No.: |
1638250-96-0 |
| 名称: |
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| 别名: |
ETC-159，ETC 159，ETC159，ETC 1922159，ETC-1922159，ETC1922159 |
| SMILES: |
C(=O)1N(C)C(=O)N(C)C2N=CN(CC(=O)NC3=CC=C(C4=CC=CC=C4)N=N3)C1=2 |
| 分子式: |
C19H17N7O3 |
| 分子量: |
391.38 |
| 纯度: |
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| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
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| In Vitro: |
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| References: |
ETC-159 is a potent and specific inhibitor of Wnt secretion. ETC-159 inhibits β-catenin reporter activity in a dose-dependent manner with an IC50 of 2.9 nM.
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.
in vivo: ETC-159 inhibits mouse PORCN with an IC50 of 18.1 nM, whereas the IC50 for Xenopus Porcn was approximately fourfold 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%. |
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MSDS
| TITLE |
DOWNLOAD |
| MSDS_2386_DC8489_1638250-96-0 |
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COA
| LOT NO. |
DOWNLOAD |
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