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ETC-159 Sale

(Synonyms: 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) 目录号 : GC19144

A potent, orally bioavailable inhibitor of PORCN

ETC-159 Chemical Structure

Cas No.:1638250-96-0

规格 价格 库存 购买数量
5mg
¥450.00
现货
10mg
¥720.00
现货
50mg
¥2,250.00
现货
100mg
¥4,050.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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实验参考方法

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].

References:

[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.

产品描述

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].

References:
[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.

Chemical Properties

Cas No. 1638250-96-0 SDF
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
Canonical SMILES O=C(NC1=CC=C(C2=CC=CC=C2)N=N1)CN3C=NC4=C3C(N(C)C(N4C)=O)=O
分子式 C19H17N7O3 分子量 391.38
溶解度 DMSO : ≥ 34 mg/mL (86.87 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.5551 mL 12.7753 mL 25.5506 mL
5 mM 0.511 mL 2.5551 mL 5.1101 mL
10 mM 0.2555 mL 1.2775 mL 2.5551 mL
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