|N-(3-((6-((3-(三氟甲基)苯基)氨基)嘧啶-4-基)氨基)苯基)环丙酰胺|CsnPharm

CAS No.: 879127-07-8

EGFR-IN-12/EGFR抑制剂 Catalog No. CSN25629

Synonyms: EGFR Inhibitor;Epidermal Growth Factor Receptor Inhibitor;ErbB-1 Inhibitor

EGFR Inhibitor is a potent, ATP-competitive and highly selective EGFR inhibitor with IC50 values of 21nM, 63nM and 4nM for EGFR, EGFR (L858R) and EGFR (L861Q), respectively. It blocked EGF-induced EGFR autophosphorylation in U-2OS cells at 10µM.

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技术信息

生物活性

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4190 mL
- 12.0949 mL
- 24.1899 mL
- 5 mM
- 0.4838 mL
- 2.4190 mL
- 4.8380 mL
- 10 mM
- 0.2419 mL
- 1.2095 mL
- 2.4190 mL

技术信息

CAS号

879127-07-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H18F3N5O

运输

蓝冰

分子量

413.40

别名

EGFR Inhibitor;Epidermal Growth Factor Receptor Inhibitor;ErbB-1 Inhibitor;HER1 Inhibitor;YUN-27078

溶解度

DMSO	80.0 mg/mL (193.5 mM)
Water	Insoluble
Ethanol	2.0 mg/mL (4.8 mM)

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EGFR-IN-12/EGFR抑制剂 Catalog No. CSN25629

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