甲磺酸厄洛替尼
- CAS号:248594-19-6
- 英文名:ERLOTINIB MESYLATE
- 中文名:甲磺酸厄洛替尼
- CBNumber:CB7677124
- 分子式:C23H27N3O7S
- 分子量:489.54
- MOL File:248594-19-6.mol
- 储存条件 :Store at -20°C
- 溶解度 :25℃: DMSO
- 形态 :Powder
甲磺酸厄洛替尼性质、用途与生产工艺
- 生物活性 Erlotinib mesylate (CP-358774 mesylate) 为 EGFR 抑制剂,IC50 值为 2 nM。
-
靶点
EGFR
2 nM (IC 50 )
-
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 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.
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体内研究
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.
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