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AZD3759 编号 : 901301

化学信息

产品英文名称AZD3759
Iupac 化学名称(R)-4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate 
同义词AZD-3759;AZD3759;AZD 3759 
英文同义词AZD-3759;AZD3759;AZD 3759 
分子式C22H23ClFN5O3 
分子量459.90 
SmileCOC1=C(OC(N2[[email protected]](C)CN(C)CC2)=O)C=C3C(N=CN=C3NC4=CC=CC(Cl)=C4F)=C1
InChiKeyMXDSJQHFFDGFDK-CYBMUJFWSA-N
InChiInChI=1S/C22H23ClFN5O3/c1-13-11-28(2)7-8-29(13)22(30)32-19-9-14-17(10-18(19)31-3)25-12-26-21(14)27-16-6-4-5-15(23)20(16)24/h4-6,9-10,12-13H,7-8,11H2,1-3H3,(H,25,26,27)/t13-/m1/s1
Cas1626387-80-1

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 6 months-80ºCin solvent 
运输条件Shipped under ambient temperature 
质量控制 HNMR HPLC

产品详情

AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. Upon oral administration, AZD3759 binds to and inhibits the activity of EGFR as well as certain mutant forms of EGFR. This prevents EGFR-mediated signaling, and may lead to both induction of cell death and inhibition of tumor growth in EGFR-overexpressing cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. Check for active clinical trials using this agent.

Reference:

1. Li X, Wang Y, Wang J, Zhang T, Zheng L, Yang Z, Xing L, Yu J.,Enhanced efficacy of AZD3759 and radiation on brain metastasis from EGFR mutant non-small cell lung cancer.Int J Cancer. 2018 Jul 1;143(1):212-224. doi: 10.1002/ijc.31303. Epub 2018 Mar 1.

2. Chao D, Pang L, Shi Y, Wang W, Liu K., AZD3759 induces apoptosis in hepatoma cells by activating a p53-SMAD4 positive feedback loop.Biochem Biophys Res Commun. 2019 Feb 5;509(2):535-540. doi: 10.1016/j.bbrc.2018.12.102. Epub 2018 Dec 28.

结构

901301 - AZD3759 | CAS 1626387-80-1

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