BI-4020 |
| Catalog No.GC38402 |
Le BI-4020 est un inhibiteur de tyrosine kinase EGFR de quatrième génération, actif par voie orale et non covalent. Le BI-4020 inhibe non seulement le variant triple mutant EGFR del19 T790M C797S (IC50 = 0,2 nM dans les lignées cellulaires BaF3), mais également le double mutant EGFR del19 T790M et le mutant primaire EGFR del19 (IC50 = 1 nM). Le BI-4020 montre également une activité contre l'EGFR wt (IC50 = 190 nM). Le BI-4020 présente une sélectivité kinome élevée et de bonnes propriétés DMPK.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2664214-60-0
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');)
;)
BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor, which inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM) whilst sparing activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties[1].
BI-4020 inhibits p-EGFR del19 T790M C797S with an IC50 of 0.6 nM[1].
BI-4020 leads to tumor regressions in the human PC-9 (EGFR del19 T790M C797S) triple mutant NSCLC xenograft model in mice[1].
[1]. Engelhardt H,et al. Start selective and rigidify: The discovery path towards a next generation of EGFR tyrosine kinase inhibitors. J Med Chem. 2019 Nov 5.
Average Rating: 5 (Based on Reviews and 13 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 *