Home Protein Tyrosine Kinase EGFR inhibitor WZ3146

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WZ3146 EGFR inhibitor

Cat.No.S1170

WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; this compound does not inhibit ERBB2 phosphorylation (T798I).
WZ3146 EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 464.95

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S117001 DMSO]93 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.73%
99.73

Chemical Information, Storage & Stability

Molecular Weight 464.95 Formula

C24H25ClN6O2

 Storage (From the date of receipt)
CAS No. 1214265-56-1 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)OC4=CC=CC(=C4)NC(=O)C=C)Cl

Solubility

In vitro
Batch:

DMSO : 93 mg/mL ( (200.02 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features
Mutant-selective, irreversible.
Targets/IC50/Ki
EGFR (L858R) [1]
2 nM
EGFR (E746_A750) [1]
2 nM
EGFR (L858R/T790M) [1]
5 nM
EGFR (E746_A750/T790M) [1]
14 nM
In vitro
WZ3146 significantly suppresses the growth of EGFR mutation containing cell lines with IC50 of 3 nM in EGFR Del E746_A750 containing HCC827 cells, 15 nM in EGFR Del E746_A750 containing PC9 cells, 29 nM in EGFR L858R/T790M containing H1975 cells and 3 nM in EGFR Del E746_A750/T790M containing PC9 GR cells. [1]
Kinase Assay
In-vitro inhibitory enzyme kinetic assays
The assays are carried out in triplicate using the ATP/NADH coupled assay system in a 96-well format. The final reaction mixture contains 0.5 mg/mL Bovine Serum Albumin (BSA), 2 mM MnCl2, 1 mM phospho(enol) pyruvic acid (PEP), 1 mM TCEP, 0.1 M Hepes 7.4, 2.5 mM poly-[Glu4Tyr1] peptide, 1/50 of the final reaction mixture volume of pyruvate kinase/lactic dehydrogenase enzymes from rabbit muscle, 0.5 mM NADH, 0.5 μM EGFR kinase, 100 μM ATP and varied amount of WZ3146. This compound and ATP are mixed and made separate stock from the mixture with all other ingredients and added last to the latter to start the reaction. Steady state initial velocity data are drawn from the slopes of the A340 curves.
References

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