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OSI-420
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。
OSI-420图片
CAS NO:183320-51-6
规格:98%
分子量:415.87
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
CAS:183320-51-6
分子式:C21H22ClN3O4
分子量:415.87
纯度:98%
存储:Store at -20°C

Background:

OSI-420 is the major metabolite of OSI-774(erlotinib) which is a small molecule, orally active, potent, and selective inhibitor of EGFR tyrosine kinase with an IC50 value of 2nM[1,2].


OSI-420 is the active metabolite of OSI-774(erlotinib) which selectively inhibits the EGFR tyrosine kinase and prevents autophosphorylation by competing with adenosine triphosphate (ATP) for its binding site on the intracellular domain of EGFR. In addition, erlotinib, is metabolized to produce ATP, has been found to be selective for EGFR and lead to the induction of apoptosis by inducing the disruption of mitochondrial effect on loss of mitochondrial membrane potential and release of cytocrome c [1, 2].


参考文献:
[1] Zhang W1, Siu LL, Moore MJ, Chen EX.Simultaneous determination of OSI-774 and its major metabolite OSI-420 in human plasma by using HPLC with UV detection. J Chromatogr B Analyt Technol Biomed Life Sci. 2005 Jan 5;814(1):143-7.
[2] Bonomi P. Erlotinib: a new therapeutic approach for non-small cell lung cancer.Expert Opin Investig Drugs. 2003 Aug;12(8):1395-401.