2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
生物活性
Description
In Vivo
In Vitro
化合物的使用
Kinase Assay
Cell Assay
Animal Administration
参考文献
JND3229 (JND-3229) is a novel highly potent, reversible EGFR C797S mutant inhibitor, potently inhibits the kinase activities of EGFRL858R/T790M and EGFRL858R/T790M/C797 with IC50 of 5.8 nM and 30.5 nM, respectively; inhibits WT EGFR with IC50 of 6.8 nM, JND3229 potently inhibits the phosphorylation of EGFRL858R/T790M/C797S and EGFR19D/T790M/C797S in a dose-dependent manner in cell-based assays, also demonstrates strong inhibition on the EGFRC797S activation in the BaF3 cells; inhibits the proliferation of BaF3 cells harboring the EGFRL858R/T790M/C797S and EGFR19D/T790M/C797S mutations with IC50 values of 0.51 and 0.32 µM, respectively; demonstrates in vivo monodrug anticancer efficacy in xenograft mouse models.
