产品说明书

AZD3759

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Chemical Structure| 1626387-80-1 同义名 : -
CAS号 : 1626387-80-1
货号 : A171107
分子式 : C22H23ClFN5O3
纯度 : 98%
分子量 : 459.901
MDL号 : -
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(108.72 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • EGFR/ErbB1

    EGFR (L858R), IC50:0.2 nM

    EGFR (WT), IC50:0.3 nM
描述 Zorifertinib (AZD3759) is a highly potent, orally bioavailable EGFR inhibitor with the ability to penetrate the central nervous system. It demonstrates remarkable efficacy against EGFR mutations, exhibiting IC50 values of 0.3 nM for wild-type EGFR (EGFRwt), 0.2 nM for EGFR with the L858R mutation (EGFRL858R), and 0.2 nM for EGFR with an exon 19 deletion (EGFRexon 19Del) at ATP concentrations equivalent to Km. Zorifertinib effectively induces apoptosis in cancer cells and shows significant antitumor activity, making it a valuable candidate for research into non-small cell lung cancer (NSCLC), hepatocellular carcinoma (HCC), and potentially other malignancies[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
H3255 cells Proliferation assay 72 h Antiproliferative against human H3255 cells expressing EGFR L858R mutant after 72 hrs by MTS assay, IC50=0.007 μM 26313252
H838 cells Function assay Inhibition of EGFR phosphorylation in human H838 cells, IC50=0.0645 μM 26313252
PC9 cells Function assay Inhibition of EGFR exon19 deletion mutant phosphorylation in human PC9 cells, IC50=0.0074 μM 26313252
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.87mL

2.17mL

1.09mL

21.74mL

4.35mL

2.17mL
参考文献

[1]Zeng Q, et al. Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. J Med Chem. 2015 Oct 22;58(20):8200-15.