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ETC-159

Cat. No. M8934
ETC-159 Structure
Synonym:

ETC-1922159

Size Price Availability Quantity
10mg USD 180  USD200 In stock
25mg USD 360  USD400 In stock
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Quality Control
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 391.38
Formula C19H17N7O3
CAS Number 1638250-96-0
Purity 99.47%
Solubility DMSO: ≥ 25 mg/mL
Storage at -20°C
References

Wnt addiction of genetically defined cancers reversed by PORCN inhibition.
Madan B, et al. Oncogene. 2016 Apr 28;35(17):2197-207. PMID: 26257057.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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