879127-07-8

Basic information

• Product Name: EGFR inhibitor
• Synonyms: EGFR inhibitor;CyclopropanecarboxaMide, N-[3-[[6-[[3-(trifluoroMethyl)phenyl]aMino]-4-pyriMidinyl]aMino]phenyl]-;EGFR Inhibitor [879127-07-8]
• CAS NO: 879127-07-8
• Molecular Formula: C21H18F3N5O
• Molecular Weight: 413.3957296
• EINECS: -0
• Product Categories: A EGFR tyrosine kinase inhibitor.
• Mol File: 879127-07-8.mol
• Article Data: 2

Chemical Properties

• Boiling Point: 605.9±55.0 °C(Predicted)
• Appearance: /
• Density: 1.456±0.06 g/cm3(Predicted)
• Solubility: insoluble in H2O; insoluble in EtOH; ≥60.7 mg/mL in DMSO
• PKA: 14.50±0.70(Predicted)
• CAS DataBase Reference: EGFR inhibitor(CAS DataBase Reference)
• NIST Chemistry Reference: EGFR inhibitor(879127-07-8)
• EPA Substance Registry System: EGFR inhibitor(879127-07-8)

Safety Data

• Hazardous Substances Data: 879127-07-8(Hazardous Substances Data)

Usage

Uses

EGFR Inhibitor is a highly selective, cell-permeable EGFR inhibitor.

Biological Activity

egfr inhibitor is a cell permeable, pyrimidine compound that selectively inhibits the egfr kinase with ic50 value of 21 nm [1].egfr is a transmembrane protein, and is a receptor for members of epidermal growth factor family. the binding of egfr with its ligands induces receptor dimerization and tyrosine autophosphorylation, and leads to cell proliferation. the overactivity of egfr tyrosine kinases is associated with a number of cancers, inhibition of egfr can downregulate antiapoptotic proteins such as surviving and upregulate proapoptotic proteins such as bim. thus, egfr inhibitor can induce cell apoptosis, resulting in anti-tumor effectivity [2].egfr inhibitor inhibited egfr kinase in vitro and blocks receptor autophosphorylation in cells. egfr inhibitor also inhibited l858r and l861q egfr mutants with ic50 values of 63 and 4 nm, respectively [1].

references

1. q. zhang, y. liu, f. gao, et al. discovery of egfr selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. journal of the american chemical society 128(7), 2182-2183 (2006). 2. f. ciardiello, g. tortora. egfr antagonists in cancer treatment. new england journal of medicine 358(11), 1160-1174 (2008).

Upstream product

• 99-09-2 3-nitro-aniline 
• 98-16-8 3-trifluoromethylaniline 
• 101946-39-8 N-(3-nitrophenyl) cyclopropanecarboxamide 
• 879127-21-6 N-(3-aminophenyl)-cyclopropanecarboxamide 
• 872510-82-2 (6-chloro-pyrimidin-4-yl)-(3-trifluoromethyl-phenyl)-amine 

Relevant articles and documents

COMPOUNDS AND COMPOSITIONS FOR PROTEIN KINASE INHBITORS

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly di