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Crenigacestat (LY3039478)

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

Crenigacestat (LY3039478)
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
100mg$700Check With Us
250mg$1250Check With Us
500mg$1875Check With Us

Cat #: V4902 CAS #: 1421438-81-4 Purity ≥ 98%

Description: Crenigacestat (formerly also known as LY3039478) is a novel, potent and orally bioavailable small molecule Notch inhibitor with an IC50 of ~1nM in cell based assays.

References: Bhagat TD, et al. Notch Pathway Is Activated via Genetic and Epigenetic Alterations and Is a Therapeutic Target in Clear Cell Renal Cancer. J Biol Chem. 2017 Jan 20;292(3):837-846.

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Molecular Weight (MW)464.43763
Molecular FormulaC22H23F3N4O4
CAS No.1421438-81-4
Storage-20℃ for 3 years in powder formrr
-80℃ for 2 years in solvent
SMILES CodeO=C(N[C@@H](C)C(N[C@H]1C2=CC=CC=C2C3=CC=CN=C3N(CCO)C1=O)=O)CCC(F)(F)F
SynonymsLY3039478; LY 3039478; LY-3039478
ProtocolIn VitroCrenigacestat (LY3039478) decreases expression of Myc and cyclin A1 (part of the NOTCH-driven proliferative signature) in murine and human model systems. Crenigacestat (LY3039478) treatment also leads to G0/G1 cell cycle arrest in CCRCC cells
In VivoCrenigacestat (8 mg/kg, oral gavage three times a week) resulted in significantly increases survival and delayed tumor growth in independent cohorts of mice demonstrating in vivo efficacy in CCRCC
Animal modelCCRCC xenografts were established in NOD-scid IL2R null mice with subcutaneous implantation using the 769-P cell line
Dosages8 mg/kg
AdministrationOral gavage three times a week.
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
1mM2.1531 mL10.7657 mL21.5314 mL43.0628 mL
5mM0.4306 mL2.1531 mL4.3063 mL8.6126 mL
10mM0.2153 mL1.0766 mL2.1531 mL4.3063 mL
20mM0.1077 mL0.5383 mL1.0766 mL2.1531 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
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.