EGFR-IN-12

产品说明书

Print
Chemical Structure| 879127-07-8 同义名 : EGFR Inhibitor;Epidermal Growth Factor Receptor Inhibitor;YUN27078;HER1 Inhibitor;ErbB-1 Inhibitor
CAS号 : 879127-07-8
货号 : A1209298
分子式 : C21H18F3N5O
纯度 : 99%+
分子量 : 413.396
MDL号 : MFCD13191284
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(604.75 mM)，配合低频超声助溶，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, IC50:21 nM
描述 The epidermal growth factor receptor (EGFR) tyrosine kinase was one of the first receptor tyrosine kinases to be targeted for drug development by the pharmaceutical industry due to its ubiquitous overexpression in a variety of tumors. EGFR Inhibitor is a highly selective inhibitor of the EGFR with an IC50 of 21 nM against EGFR kinase in vitro and blocks receptor autophosphorylation in cells. It exhibits exclusive selectivity against EGFR at a concentration of 10 μM and potently inhibits two EGFR mutants associated with clinical response to gefitinib: L858R (IC50 = 63 nM) and L861Q (IC50 = 4 nM). Treatment of U-2OS cells transfected with WT EGFR with epidermal growth factor (EGF) resulted in receptor autophosphorylation. Pretreatment of cells with EGFR Inhibitor (10 μM) resulted in complete inhibition of WT receptor autophosphorylation. This result was also evident from the observation that greater levels of receptor were immunoprecipitated from compound-treated compared to untreated cells, consistent with reports that EGFR activation leads to its rapid degradation[1].
作用机制 The selectivity of EGFR Inhibitor is derived from the ability to form three hydrogen bonding interactions while occupying a hydrophobic cavity made accessible due to the small gatekeeper threonine 766[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.09mL

2.42mL

1.21mL

24.19mL

4.84mL

2.42mL
参考文献

[1]Zhang Q, Liu Y, Gao F, et al. Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. J Am Chem Soc. 2006;128(7):2182-2183