La description
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.ÂÂ
AbstractÂÂ
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.
| Pays: |
China |
| N ° de modèle: |
-
|
| Prix FOB: |
(Negotiable)
Obtenir le dernier prix
|
| Localité: |
- |
| Prix de commande minimale: |
- |
| Commande minimale: |
- |
| Packaging Detail: |
- |
| Heure de livraison: |
- |
| Capacité de Fournir: |
- |
| Payment Type: |
- |
| Groupe de produits : |
alkaloid oncology medicine
|
