EGFR Inhibitor (Synonyms: Epidermal Growth Factor Receptor Inhibitor) |
| Catalog No.GC11312 |
El inhibidor de EGFR es una pirimidina disustituida en 4,6 y es un inhibidor de EGFR potente, competitivo con ATP, irreversible y altamente selectivo con una IC50 de 21 nM. El inhibidor de EGFR también inhibe los mutantes EGFRL858R y EGFRL861Q con IC50 de 63 nM y 4 nM, respectivamente. El inhibidor de EGFR muestra una fuerte selectividad por EGFR sobre HER4 (IC50 = 7640 nM) y un panel de otras 55 quinasas. El inhibidor de EGFR induce la apoptosis de las células y tiene actividad antitumoral.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 879127-07-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
EGFR inhibitor is a cell permeable, pyrimidine compound that selectively inhibits the EGFR kinase with IC50 value of 21 nM [1].
EGFR is a transmembrane protein, and is a receptor for members of epidermal growth factor family. The binding of EGFR with its ligands induces receptor dimerization and tyrosine autophosphorylation, and leads to cell proliferation. The overactivity of EGFR tyrosine kinases is associated with a number of cancers, inhibition of EGFR can downregulate antiapoptotic proteins such as surviving and upregulate proapoptotic proteins such as Bim. Thus, EGFR inhibitor can induce cell apoptosis, resulting in anti-tumor effectivity [2].
EGFR inhibitor inhibited EGFR kinase in vitro and blocks receptor autophosphorylation in cells. EGFR inhibitor also inhibited L858R and L861Q EGFR mutants with IC50 values of 63 and 4 nM, respectively [1].
References:
1. Q. Zhang, Y. Liu, F. Gao, et al. Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. Journal of the American Chemical Society 128(7), 2182-2183 (2006).
2. F. Ciardiello, G. Tortora. EGFR antagonists in cancer treatment. New England Journal of Medicine 358(11), 1160-1174 (2008).
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *