埃罗替尼甲磺酸盐  ≥98%

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包装规格:100mg 500mg in glass bottle
产品简介:一种为EGFR 抑制剂,IC50 值为 2nM。
靶点:EGFR:2 nM (IC50)
体外研究:Erlotinib mesylate (CP-358774 mesylate) is also a potent inhibitor of the recombinant intracellular (kinase) domain of the EGFR, with an IC50 of 1 nM. The proliferation of DiFi cells is strongly inhibited by Erlotinib with an IC50 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.
体内研究:There is a 1.49-fold statistically significant difference between AUC0-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.
保存条件:-20℃
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