WZ3146

Names

[ Name ]:
WZ3146

[Synonym ]:
N-{3-[(5-Chloro-2-{[4-(4-methyl-1-piperazinyl)phenyl]amino}-4-pyrimidinyl)oxy]phenyl}acrylamide
WZ-3146,WZ3146
S1170_Selleck
2-Propenamide, N-[3-[[5-chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-
CS-0111
N-(3-(5-chloro-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)acrylamide
WZ-3146
cc-597

Biological Activity

[Description]:

WZ3146 is a mutant selective EGFR inhibitor with IC50s of 2, 2, 5, 14 and 66 nM for EGFRL858R, EGFRL858R/T790M, EGFRE746_A750, EGFRE746_A750/T790M and EGFR, respectively.

[Related Catalog]:

Research Areas >> Cancer

[Target]

EGFRL858R:2 nM (IC50)

EGFRL858R/T790M:5 nM (IC50)

EGFRE746_A750:2 nM (IC50)

EGFRE746_A750/T790M:14 nM (IC50)

EGFR:24 nM (IC50)

[In Vitro]

WZ3146 is a novel EGFR inhibitor, suppresses the growth of EGFR T790M containing cell lines and inhibits EGFR phosphorylation[1].

[Kinase Assay]

In vitro inhibitory enzyme kinetic assays are carried out in triplicate using the ATP/NADH coupled assay system in a 96-well format. The final reaction mixture contains 0.5mg/mL Bovine Serum Albumin (BSA), 2mM MnCl2, 1mM phospho(enol) pyruvic acid, 1mM TCEP, 0.1M Hepes 7.4, 2.5mM poly-[Glu4Tyr1] peptide, 1/50 of the final reaction mixture volume of pyruvate kinase/lactic dehydrogenase enzymes from rabbit muscle, 0.5mM NADH, 0.5μM EGFR kinase, 100μM ATP and varied amount of inhibitors. Inhibitors 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[1].

[Animal admin]

Growth and inhibition of growth is assessed by MTS assay. Ba/F3 cells are exposed to WZ3146 treatment for 72 hours. Growth and inhibition of growth is assessed by MTS assay[1].

[References]

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

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C₂₄H₂₅ClN₆O₂

[ Molecular Weight ]:
464.947

[ Exact Mass ]:
464.172760

[ PSA ]:
86.11000

[ LogP ]:
3.60

[ Index of Refraction ]:
1.661

[ Storage condition ]:
-20℃

WZ3146

Names

Biological Activity

Chemical & Physical Properties

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds