[CAS NO. 1638250-96-0] ETC-159
PRODUCTS SPECIFICATIONS [1638250-96-0]
DESCRIPTION [1638250-96-0]
Overview
| MDL | MFCD29472267 |
|---|---|
| Molecular Weight | 391.38 |
| Molecular Formula | C19H17N7O3 |
| SMILES | O=C(NC1=CC=C(C2=CC=CC=C2)N=N1)CN3C=NC4=C3C(N(C)C(N4C)=O)=O |
3 Publications Citing Use of MCE
Summary
ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. ETC-159 inhibits β-catenin reporter activity with an IC 50 of 2.9 nM.
IC50 & Target
IC50: 2.9 nM (β-catenin) [1]
In Vitro
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]
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ETC-159 inhibits mouse PORCN with an IC 50 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 T max of ~0.5 h and oral bioavailability of 100% [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02521844 | EDDC (Experimental Drug Development Centre), A*STAR Research Entities|PPD |
Solid Tumors
|
October 2015 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 127.75 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution