BI-4020 |
| Catalog No.GC38402 |
BI-4020 es un inhibidor de la tirosina quinasa EGFR de cuarta generaciÓn, activo por vÍa oral y no covalente. BI-4020 inhibe no solo la variante triple mutante EGFR del19 T790M C797S (IC50 = 0,2 nM en lÍneas celulares BaF3), sino también el doble mutante EGFR del19 T790M y el mutante primario EGFR del19 (IC50 = 1 nM). BI-4020 también muestra actividad frente a EGFR wt (IC50=190 nM). BI-4020 muestra una alta selectividad de kinomas y buenas propiedades de 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 *