貨號	規格	價格	上海	北京	武漢	南京
S83776-5mg	98.8%	￥370.00 S83776-5mg ￥370.00 現貨	5 5	-	-	-
S83776-10mg	98.8%	￥640.00 S83776-10mg ￥640.00 現貨	7 7	-	-	-
S83776-25mg	98.8%	￥900.00 S83776-25mg ￥900.00 現貨	4 4	-	-	-
S83776-100mg	98.8%	￥2600.00 S83776-100mg ￥2600.00 現貨	3 3	-	-	-

產品介紹

ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. ETC-159 inhibits β-catenin reporter activity with an IC50 of 2.9 nM

產品描述：

ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. ETC-159 inhibits β-catenin reporter activity with an IC50 of 2.9 nM

靶點：

IC50: 2.9 nM (β-catenin);Wnt/beta-catenin;?Porcupine

體外研究：

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。

體內研究：

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%。

參考文獻：

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.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.555 ml	12.775 ml	25.55 ml
5 mM	0.511 ml	2.555 ml	5.11 ml
10 mM	0.256 ml	1.278 ml	2.555 ml
50 mM	0.051 ml	0.256 ml	0.511 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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