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Purity: ≥98%
ETC-159 (ETC-192215) is a novel, potent and orally bioavailable PORCN inhibitor which inhibits β-catenin reporter activity with an IC50 of 2.9 nM and 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. ETC-159 is remarkably effective in treating RSPO-translocation bearing colorectal cancer (CRC) patient-derived xenografts.
| ln Vitro |
All Wnt activity and secretion are inhibited by ETC-159. Strong activity of ETC-159 is seen in several cancer models with elevated Wnt signaling. When R-spondin translocations are present in colorectal cancers (CRCs), which are defined molecularly, ETC-159 is very effective[1].
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| ln Vivo |
With an IC50 of 18.1 nM, ETC-159 inhibits mouse PORCN, while Xenopus Porcn has an IC50 that is roughly four times higher (70 nM). When used to treat xenografts derived from patients with colorectal cancer (CRC) that bear RSPO-translocation, ETC-159 shows remarkable efficacy. ETC-159 shows favorable oral pharmacokinetics in mice, enabling oral administration for preclinical assessment. ETC-159 has an oral bioavailability of 100% and a Tmax of approximately 0.5 hours after a single dose of 5 mg/kg, which is rapidly absorbed into the blood [1].
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| Additional Infomation |
Porcupine Inhibitor ETC-1922159 is an orally bioavailable inhibitor of the membrane-bound O-acyltransferase (MBOAT) porcupine (PORCN), with potential antineoplastic activity. Upon oral administration, ETC-1922159 binds to and inhibits PORCN in the endoplasmic reticulum (ER), which blocks post-translational palmitoylation of Wnt ligands and inhibits their secretion. This prevents the activation of Wnt ligands, interferes with Wnt-mediated signaling, and inhibits cell growth in Wnt-driven tumors. Porcupine catalyzes the palmitoylation of Wnt ligands, and plays a key role in Wnt ligand secretion. Wnt signaling is dysregulated in a variety of cancers.
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| Molecular Formula |
C19H17N7O3
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| Molecular Weight |
391.38
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| Exact Mass |
391.139
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| CAS # |
1638250-96-0
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| Related CAS # |
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| PubChem CID |
86280523
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.732
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| LogP |
1.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
654
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QTRXIFVSTWXRJJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17N7O3/c1-24-17-16(18(28)25(2)19(24)29)26(11-20-17)10-15(27)21-14-9-8-13(22-23-14)12-6-4-3-5-7-12/h3-9,11H,10H2,1-2H3,(H,21,23,27)
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| Chemical Name |
2-(1,3-dimethyl-2,6-dioxopurin-7-yl)-N-(6-phenylpyridazin-3-yl)acetamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5551 mL | 12.7753 mL | 25.5506 mL | |
| 5 mM | 0.5110 mL | 2.5551 mL | 5.1101 mL | |
| 10 mM | 0.2555 mL | 1.2775 mL | 2.5551 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Development of novel PORCN inhibitors.Oncogene.2016 Apr 28;35(17):2197-207. |
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 ETC-159 is orally bioavailable and effectively inhibits the growth of mouse mammary tumor virus (MMTV)-Wnt1 tumors.Oncogene.2016 Apr 28;35(17):2197-207. |
 ETC-159 inhibits Wnt autocrine signaling and growth of teratocarcinomas.Oncogene.2016 Apr 28;35(17):2197-207. |
 ETC-159 prevents growth of colorectal tumors with RSPO fusions:Oncogene.2016 Apr 28;35(17):2197-207. |
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 Global remodeling of gene expression in ETC-159 treated colon cancers with RSPO translocations.Oncogene.2016 Apr 28;35(17):2197-207. |
 Treatment with ETC-159 prevents growth of RNF43 mutant pancreatic tumors and induces differentiation.Oncogene.2016 Apr 28;35(17):2197-207. |
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