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Sapitinib(AZD8931) 编号 : 60301

化学信息

产品英文名称Sapitinib(AZD8931)
Iupac 化学名称2-(4-((4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)piperidin-1-yl)-N-methylacetamide 
同义词Sapitinib;AZD8931;AZD-8931 
英文同义词Sapitinib;AZD8931;AZD-8931 
分子式C23H25ClFN5O3 
分子量473.93 
SmileO=C(CN1CCC(OC2=CC3=C(NC4=CC=CC(Cl)=C4F)N=CN=C3C=C2OC)CC1)NC
InChiKeyDFJSJLGUIXFDJP-UHFFFAOYSA-N
InChiInChI=1S/C23H25ClFN5O3/c1-26-21(31)12-30-8-6-14(7-9-30)33-20-10-15-18(11-19(20)32-2)27-13-28-23(15)29-17-5-3-4-16(24)22(17)25/h3-5,10-11,13-14H,6-9,12H2,1-2H3,(H,26,31)(H,27,28,29)
Cas848942-61-0

技术数据

外观off-white solid 
纯度99% by HPLC 
可溶性Soluble in DMSO 
存储3 years -20ºCpowder 
运输条件Shipped under ambient temperature 
质量控制 HNMR HPLC

产品详情

AZD8931(Sapitinib)is a novel potent reversible small molecule epidermal growth factor receptor, ERBB2 (HER2) and ERBB3 inhibitor with an IC50 of 4, 3, 4 nM, respectively. In proliferation assays, AZD8931 was significantly more potent than gefitinib or lapatinib in specific squamous cell carcinoma of the head and neck and non-small cell lung carcinoma cell lines. In vivo, AZD8931 inhibited xenograft growth in a range of models while significantly affecting EGFR, erbB2, and erbB3 phosphorylation and downstream signaling pathways, apoptosis, and proliferation. It has a unique pharmacologic profile providing equipotent inhibition of EGFR, erbB2, and erbB3 signaling and showing greater antitumor activity than agents with a narrower spectrum of erbB receptor inhibition in specific preclinical models.

 

结构

60301 - Sapitinib(AZD8931) | CAS 848942-61-0

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