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Erlotinib mesylate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Erlotinib mesylate图片
CAS NO:248594-19-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
埃罗替尼甲磺酸盐
CP-358774 mesylate
NSC 718781 mesylate
OSI-774 mesylate
产品介绍
Erlotinib mesylate (CP-358774 mesylate) 为EGFR抑制剂,IC50值为 2 nM。
生物活性

Erlotinib mesylate (CP-358774 mesylate) inhibits purifiedEGFRkinase with anIC50of 2 nM.

IC50& Target[1]

EGFR

2 nM (IC50)

体外研究
(In Vitro)

Erlotinib mesylate (CP-358774 mesylate) is also a potent inhibitor of the recombinant intracellular (kinase) domain of the EGFR, with an IC50of 1 nM. The proliferation of DiFi cells is strongly inhibited by Erlotinib with an IC50of 100 nM for an 8-day proliferation assay[1]. 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[2].

体内研究
(In Vivo)

There is a 1.49-fold statistically significant difference between AUC0-infafter 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)[3]. 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[4].

Clinical Trial
分子量

489.54

Formula

C23H27N3O7S

CAS 号

248594-19-6

中文名称

埃罗替尼甲磺酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.