248594-19-6
基本信息
埃羅替尼甲磺酸鹽
Erlotinib (OSI-744) mesylate
Erlotinib mesylate (CP-358774
CP-358774
OSI-774
NSC 718781
R 1415
TARCEVA
CP-358774
OSI-774
NSC 718781
R 1415
常見問題列表
EGFR 2 nM (IC 50 ) |
Erlotinib mesylate (CP-358774 mesylate) is also a potent inhibitor of the recombinant intracellular (kinase) domain of the EGFR, with an IC 50 of 1 nM. The proliferation of DiFi cells is strongly inhibited by Erlotinib with an IC 50 of 100 nM for an 8-day proliferation assay. The combination of B-DIM and Erlotinib (2 μM) results in a significant inhibition of colony formation in BxPC-3 cells when compared with either agent alone. The combination of B-DIM and Erlotinib (2 μM) results in a significant induction of apoptosis only in BxPC-3 cells when compare with the apoptotic effect of either agent alone.
There is a 1.49-fold statistically significant difference between AUC 0-inf after p.o. administration of Erlotinib (5 mg/kg) comparing Bcrp1/Mdr1a/1b -/- and WT mice (7,419±1,720 versus 4,957±1,735 ng*h/mL respectively, P=0.01). The administration of Erlotinib (10 mg/kg/day, or 20 mg/kg/day) to Bleomycin (BLM)-treated rats shows no exacerbation of lung injuries in indices such as macroscopic findings, lung weights, histopathological scores (lung lesion density and lung fibrosis score), and pulmonary hydroxyproline (HyP) level. The result suggests that Erlotinib does not have any exacerbating effects on lung injuries induced by BLM in rats.