WZ3146

Item no.	S1170-200
Manufacturer	Selleckchem
CASRN	1214265-56-1
Amount	200 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 ml 200 mg 5 mg 50 mg 5 g
Category	Oncology Neuroscience Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer
Type	Inhibitors
Specific against	other
Smiles	CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)OC4=CC=CC(=C4)NC(=O)C=C)Cl
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	1214265-56-1'
Similar products	WZ3146
Available
Manufacturer - Targets	EGFR
Storage Conditions	2 years -80 in solvent
Molecular Weight	464, 95
Cell lines	NSCLC and Ba/F3 cells
Concentrations	0-10 uM
IC50	2 nM, 2 nM, 2 nM, 2 nM, 2 nM, 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]
Incubation Time	72 hours
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 uM EGFR kinase, 100 uM 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.
Method	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.
Solubility (25C)	DMSO 93 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	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).
Chemical Name	N-(3-(5-chloro-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)acrylamide
Features	Mutant-selective, irreversible

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