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BIBX 1382
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。
BIBX 1382图片
CAS NO:196612-93-8
规格:98%
分子量:387.84
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
EGFR inhibitor,potent and selective
CAS:196612-93-8
分子式:C18H19ClFN7
分子量:387.84
纯度:98%
存储:Store at -20°C

Background:

BIBX1382 is a potent, selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase with IC50 value of 3 nM.[1]


BIBX1382 is an inhibitor of EGFR kinase for treatment of cancer. In a tyrosine kinase activity assay using cytoplasmic tyrosine kinase domains of EGFR, HER2, VEGFR2, HGFR, IGF1R, B-InsRK and c-src cloning and expressing in Sf9 insect cells, BIBX1382 selectively and potently inhibited EGFR kinase activity with an IC50 value of 3 nM. In the EGFR and pEGFR ELISA assay using EGFR highly expressed A431 cells (vuval squamous cell carcinoma), BIBX1382 inhibited EGFR phosphorylation at EC50 at 141 nM.[1] In A431, FaDu (hypopharyngeal squamous cell carcinoma) and HN5 (head and neck squamous cell carcinoma) xenograft nude mice models, oral administration of BIBX1382 at dose of 10 mg/kg daily showed strong antitumor activity in a dose-dependent manner after 2 weeks of treatment. Moreover, tumor regressions were obtained after 170 days’ long term oral administration of BIBX1382 at dose of 50 mg/kg daily in A431 xenograft nice model.[1]


参考文献:
1. F. F. Solca, A. Baum, E. Langkopf, G. Dahmann, K. H. Heider, F. Himmelsbach and J. C. van Meel, J Pharmacol Exp Ther 2004, 311, 502-509.