甲磺酸厄洛替尼
中文名称 | 甲磺酸厄洛替尼 |
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中文同义词 | 甲磺酸厄洛替尼;埃罗替尼甲磺酸盐;化合物 T0373L1;甲磺酸埃罗替尼 |
英文名称 | ERLOTINIB MESYLATE |
英文同义词 | ERLOTINIB MESYLATE;Erlotinib (OSI-744) mesylate;TARCEVA; CP-358774; OSI-774; NSC 718781; R 1415;Erlotinib mesylate (CP-358774;CP-358774;OSI-774;NSC 718781;R 1415;CP-358 |
CAS号 | 248594-19-6 |
分子式 | C23H27N3O7S |
分子量 | 489.54 |
EINECS号 | |
相关类别 | |
Mol文件 | 248594-19-6.mol |
结构式 |
甲磺酸厄洛替尼 性质
储存条件 | Store at -20°C |
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溶解度 | 25℃:二甲基亚砜 |
形态 | 粉末 |
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.