ETC159 (ETC192215)

This product is for research use only, not for human use. We do not sell to patients.

ETC159 (ETC192215)
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Size Price Stock
500mg$1150Check With Us
1g$1850Check With Us
5g$5530Check With Us

Cat #: V2938 CAS #: 1638250-96-0 Purity ≥ 98%

Description: 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.

References: Madan B, et al. Wnt addiction of genetically defined cancers reversed by PORCN inhibition. Oncogene. 2015 Aug 10. doi: 10.1038/onc.2015.280.

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Molecular Weight (MW)391.38
Molecular FormulaC19H17N7O3
CAS No.1638250-96-0
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: ≥ 34 mg/mLr
Water: <1 mg/mLr
Ethanol: <1 mg/mL
SynonymsETC-1922159; ETC 1922159; ETC1922159; ETC-159; ETC159; ETC 159
ProtocolIn VitroETC-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
In VivoETC-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%
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.5551 mL12.7753 mL25.5506 mL51.1012 mL
5mM0.5110 mL2.5551 mL5.1101 mL10.2202 mL
10mM0.2555 mL1.2775 mL2.5551 mL5.1101 mL
20mM0.1278 mL0.6388 mL1.2775 mL2.5551 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
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Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid 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 master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (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.