ETC-159

A potent, orally bioavailable inhibitor of PORCN

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库存: 现货

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5mg

￥550.00

440.00

- +
10mg

￥875.00

700.00

- +
50mg

￥2725.00

2180.00

- +
100mg

￥4850.00

3880.00

- +

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货号: ajci22530
CAS: 1638250-96-0
别名: 1,2,3,6-四氢-1,3-二甲基-2,6-二氧代-N-(6-苯基-3-哒嗪基)-7H-嘌呤-7-乙酰胺,ETC-1922159
分子式: C19H17N7O3
分子量: 391.38
纯度: >98%
溶解度: DMSO : ≥ 34 mg/mL (86.87 mM)
储存: Store at -20°C
库存: 现货

Background

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

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]

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].

参考文献:
[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.

Protocol

Cell experiment:

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[1].

Animal experiment:

Mice: For human xenograft models, patient-derived solid tissue fragments are subcutaneously implanted in BALB/c nude mice. All groups are matched for tumor size with equal variance before treatment. ETC-159 formulated in 50% PEG400 (vol/vol) in water is administered by oral gavage at a dosing volume of 10?μL/g body weight[1].

参考文献:

[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.