WZ4002

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

WZ4002
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
500mg$450Check With Us
1g$750Check With Us
5g$1900Check With Us

Cat #: V0552 CAS #: 1213269-23-8 Purity ≥ 98%

Description: WZ4002 (WZ-4002) is a covalent/irreversible and mutant-selective EGFR (e.g. L858R/T790M) inhibitor with potential antitumor activity.

References: Zhou W, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.Nature. 2009 Dec 24;462(7276):1070-4.

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Molecular Weight (MW)494.18
Molecular FormulaC25H27ClN6O3
CAS No.1213269-23-8
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 13 mg/mL (26.3 mM)r
Water: <1 mg/mLr
Ethanol: <1 mg/mL
Solubility In Vivo30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
SMILES CodeC=CC(NC1=CC=CC(OC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3OC)=NC=C2Cl)=C1)=O
SynonymsWZ-4002; WZ 4002; WZ4002;
ProtocolIn VitroWZ4002 increases cellular potency correlated with inhibition of EGFR, AKT and ERK1/2 phosphorylation in NSCLC cell lines and EGFR phosphorylation in NIH-3T3 cells expressing different EGFRT790M mutant alleles. WZ4002 inhibits EGFR kinase activity of recombinant L858R/T790M protein more potently than of WT EGFR.
In VivoIn a pharmacodynamic study WZ4002 effectively inhibits EGFR, AKT and ERK1/2 phosphorylation which is associated with a significant increase in TUNEL positive and a significant decrease in Ki67 positive cells compared to vehicle alone treated mice. In a 2 week efficacy study, WZ4002 treatment results in significant tumor regressions compared to vehicle alone in both T790M containing murine models. Histological evaluation of the lungs following treatment confirms significant resolution of the tumor nodules with only few small residual nodules and nodule remnants that has evidence of treatment effect with decreased cellularity and increased fibrosis consistent with remodeling/scarring.
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
1mM2.0236 mL10.1178 mL20.2355 mL40.4711 mL
5mM0.4047 mL2.0236 mL4.0471 mL8.0942 mL
10mM0.2024 mL1.0118 mL2.0236 mL4.0471 mL
20mM0.1012 mL0.5059 mL1.0118 mL2.0236 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.