A cell permeable

EGFR Inhibitor – 5 mg

Brand:
Cayman
CAS:
879127-07-8
Storage:
-20
UN-No:
Non-Hazardous - /

EGFR inhibitor is a cell permeable, 4,6-disubstituted pyrimidine compound that selectively inhibits the EGFR kinase with an IC50 value of 21 nM in vitro and blocks receptor autophosphorylation in cells.{25289} It can also inhibit the L858R and L861Q EGFR mutants (IC50s = 63 and 4 nM, respectively) yet displays strong selectivity for EGFR against a panel of 55 recombinant kinases (IC50s > 10 μM).{25289} Whereas overactivity of EGFR tyrosine kinases has been associated with a number of cancers, inhibition of EGFR has been shown to induce apoptosis by downregulating antiapoptotic proteins such as survivin and upregulating proapoptotic proteins such as Bim.{25291,25290}  

 

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Description

A cell permeable, selective inhibitor of the EGFR kinase (IC50s = 21, 63, and 4 nM for EGFR and the L858R and L861Q EGFR mutants, respectively)

Formal name: N-[3-[[6-[[3-(trifluoromethyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-cyclopropanecarboxamide

Synonyms:  Epidermal Growth Factor Receptor Inhibitor

Molecular weight: 413.4

CAS: 879127-07-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cell Biology|Cell Death|Apoptosis||Research Area|Cell Biology|Cell Signaling|ERK/MAPK Signaling

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