Descripción del producto

WZ***2,*********8

1. WZ***2, a thirdgeneration EGFR inhibitor, can overcome anoikis resistance in EGFRmutant lung adenocarcinomas more efficiently than Src inhibitors. Lab Invest. ***2 Mar;*2(3):****3. doi: *0.***8/labinvest.***1.**7. Epub ***1 Dec *2. 
Abstract 
Due to the ability of WZ***2, an EGFR TKI, to suppress phosphorylated EGFR in both H***5 and HCC**7 cells, the combination of WZ***2, ABT**3 and TSA almost completely eradicated both the suspended cell lines.

WZ***2 is a novel mutantselective epidermal growth factor receptor (EGFR) kinase inhibitor that potently and irreversibly suppresses the ATPdependent autophosphorylation of both wildtype EGFR and EGFR mutants, including EGFR delE**6_A**0/T**0M, EGFR L**8R/T**0M, EGFR T**0M, EGFR delE**6_A**0 and EGFR L**8R, with inhibition constant Ki of *3.6 nM, 1.8 nM, 4 nM, 5 nM, 3.9 nM and 8.5 nM respectively. Although WZ***2 is actively against EGFR mutants rather than wildtype EGFR at lower concentrations resulting in less toxicity in normal tissues, wildtype EGFR is susceptible to higher concentrations of WZ***2 as well as prolonged administration of WZ***2, especially in tissues where it accumulates.

References:
[1]Lee HJ, Schaefer G, Heffron TP, Shao L, Ye X, Sideris S, Malek S, Chan E, Merchant M, La H, Ubhayakar S, Yauch RL, Pirazzoli V, Politi K, Settleman J. Noncovalent wildtypesparing inhibitors of EGFR T**0M. Cancer Discov. ***3 Feb;3(2):****1. doi: *0.***8/*******0.CD*****7. Epub ***2 Dec *0.
[2]Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Jnne PA. Novel mutantselective EGFR kinase inhibitors against EGFR T**0M. Nature. ***9 Dec *4;**2(***6):****4. doi: *0.***8/nature****2.
[3]Zannetti A, Iommelli F, Speranza A, Salvatore M, Del Vecchio S. 3'deoxy3'*8Ffluorothymidine PET/CT to guide therapy with epidermal growth factor receptor antagonists and BclxL inhibitors in nonsmall cell lung cancer. J Nucl Med. ***2 Mar;*3(3):****0. doi: *0.***7/jnumed.**1.*****3. Epub ***2 Feb *3.