Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC 50 of 5 nM; also inhibits mutant EGFR L858R , EGFR L858R/T790M , EGFR T790M and EGFR L861Q .
In Vitro
Incubation with Iconitib at 0.5 μM results in kinase activity inhibition of 91%, 99%, 96%, 61% and 61%, respectively. Iconitib inhibits the proliferation of A431 and BGC-823 A549, H460 and KB cell lines with IC 50 s of 1, 4.06, 12.16, 16.08, 40.71 μM. When profiled with 88 kinases, Icotinib only shows meaningful inhibitory activity to EGFR and its mutants. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation (IC 50 =45 nM) in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Icotinib exhibits potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug is well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment. Icotinib inhibits tumor growth at a rate of 25.2%, 45.6% and 51.5% in the A431 cell line groups; 3.4%, 25.9% and 31.0% in the A549 cell line groups; 49.4%, 52.6% and 67.4% in the H460 cell line groups, and 30.3%, 36.4% and 46.5% in the HCT8 cell line groups, at 30, 60 and 120 mg/kg/dose, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:EGFR 5 nM (IC 50 ) EGFR L861Q EGFR L858R/T790M EGFR L858R EGFR T790M
