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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Porcupine-ECT-159
ECT-159

Chemical Structure : ECT-159

CAS No.: 1638250-96-0

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ECT-159 (ETC-1922159, ECT159)

货号: PC-72828Not For Human Use, Lab Use Only.

ECT-159 (ETC-1922159) is a potent, orally available Porcupine (PORCN) inhibitor that blocks the secretion and activity of all Wnts, inhibits β-catenin reporter activity with IC50 of 2.9 nM.

规格 价格 库存 数量
10 mg ￥780 In stock
25 mg ￥1280 In stock
50 mg ￥2180 In stock
100 mg ￥3580 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ECT-159 (ETC-1922159) is a potent, orally available Porcupine (PORCN) inhibitor that blocks the secretion and activity of all Wnts, inhibits β-catenin reporter activity with IC50 of 2.9 nM.
ECT-159 effectively inhibited the secretion of WNT3A into culture media but did not inhibit β-catenin signaling in STF cells supplemented with Wnt3A-conditioned medium.
ETC-159 is orally bioavailable and effectively inhibits the growth of mouse mammary tumor virus (MMTV)-Wnt1 tumors, inhibits Wnt autocrine signaling and growth of teratocarcinomas, significantly reduces the phosphorylation of both Dvl2 and LRP6, prevents growth of colorectal tumors with RSPO fusions, induces global remodeling of gene expression in colon cancers with RSPO translocations.

物理化学性质&存储条件

分子量 391.391
分子式 C19H17N7O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(6-phenylpyridazin-3-yl)acetamide

参考文献

1. B Madan, et al. Oncogene. 2016 Apr 28;35(17):2197-207.

2. Madan B, et al. Bone Res. 2018 May 25;6:17.

3. Zhong Z, et al. Oncogene. 2019 Oct;38(40):6662-6677.

4. Liu Z, et al. J Med Chem. 2021 Apr 22;64(8):4257-4288.

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