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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
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
OSI-420 (OSI-420) 是厄洛替尼的活性代谢物。厄洛替尼是一种有效的 EGFR 酪氨酸激酶抑制剂。
Cas No.183320-51-6
别名OSI-420; CP-373420 hydrochloride
化学名2-[4-(3-ethynylanilino)-7-(2-methoxyethoxy)quinazolin-6-yl]oxyethanol;hydrochloride
Canonical SMILESCOCCOC1=C(C=C2C(=C1)N=CN=C2NC3=CC=CC(=C3)C#C)OCCO.Cl
分子式C21H22ClN3O4
分子量415.87
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

References:
[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.