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WZ-3146

Catalog No. T6733 CAS 1214265-56-1

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

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WZ-3146, CAS 1214265-56-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 48.00
2 mg	In stock	$ 68.00
5 mg	In stock	$ 98.00
10 mg	In stock	$ 189.00
25 mg	In stock	$ 335.00
50 mg	In stock	$ 537.00
100 mg	In stock	$ 768.00
1 mL * 10 mM (in DMSO)	In stock	$ 108.00

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Purity: 98.95%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I).
Targets&IC50	EGFR (L858R):2 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. WZ3146 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.
Cell Research	Growth and inhibition of growth is assessed by MTS assay. NSCLC or Ba/F3 cells are exposed to treatment for 72 hours and the number of cells used per experiment is determined empirically. All experimental points are set up in six to twelve wells and all experiments are repeated at least three times. The data is graphically displayed using GraphPad Prism version 5.0 for Windows. The curves are fitted using a non-linear regression model with a sigmoidal dose response.(Only for Reference)

Molecular Weight	464.95
Formula	C24H25ClN6O2
CAS No.	1214265-56-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 86 mg/mL (185 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Zhou W, et al. Nature, 2009, 462(7276), 1070-1074.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library Highly Selective Inhibitor Library Inhibitor Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Apoptosis Compound Library Bioactive Compounds Library Max Anti-Breast Cancer Compound Library Anti-Lung Cancer Compound Library Bioactive Compound Library

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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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

WZ-3146 1214265-56-1 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR HER1 Epidermal growth factor receptor WZ3146 WZ 3146 ErbB-1 inhibit Inhibitor inhibitor

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