1214265-56-1

1214265-56-1 structure

Name: WZ3146
Chemical Name: N-[3-[5-chloro-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]prop-2-enamide
CAS Number: 1214265-56-1
Molecular Formula: C₂₄H₂₅ClN₆O₂
Molecular Weight: 464.947
Catalog: Biochemical Inhibitor Protein tyrosine kinase
Create Date: 2017-01-06 05:05:25
Modify Date: 2024-01-03 16:38:16
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.

Name	N-[3-[5-chloro-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]prop-2-enamide
Synonyms	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

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.

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℃