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ETC-159

Cat. No. M8934
ETC-159 Structure
Synonym:

ETC-1922159

Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 80  USD80 In stock
25mg USD 150  USD150 In stock
50mg USD 250  USD250 In stock
100mg USD 450  USD450 In stock
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Quality Control & Documentation
Biological Activity

ETC-159 is a potent, selective and orally available PORCN inhibitor, which 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 remarkably effective in treating RSPO-translocation bearing colorectal cancer (CRC) patient-derived xenografts. 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 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%

Protocol (for reference only)
Cell Experiment
Cell lines HEK293 cells, STF3A cells
Preparation method 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.
Concentrations 100 nm
Incubation time 24 h
Animal Experiment
Animal models Mice
Formulation Formulated in 50% PEG400 (vol/vol) in water
Dosages 10 μL/g
Administration oral gavage
Chemical Information
Molecular Weight 391.38
Formula C19H17N7O3
CAS Number 1638250-96-0
Solubility (25°C) DMSO: ≥ 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Madan B, et al. Oncogene. Wnt addiction of genetically defined cancers reversed by PORCN inhibition.

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  Catalog
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Keywords: ETC-159, ETC-1922159 supplier, Wnt/beta-catenin, inhibitors, activators


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