EGFR-IN-12 (Standard)

EGFR-IN-12 (Standard) is the analytical standard of EGFR-IN-12. This product is intended for research and analytical applications. EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFRL858R and EGFRL861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity[1][2].

Product Specifications

CAS Number

[879127-07-8]

UNSPSC

12352100

Target

Apoptosis; EGFR; Reference Standards

Related Pathways

Apoptosis; JAK/STAT Signaling; Others; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Smiles

O=C(C1CC1)NC2=CC=CC(NC3=NC=NC(NC4=CC=CC(C(F)(F)F)=C4)=C3)=C2

Molecular Formula

C21H18F3N5O

Molecular Weight

413.40

References & Citations

[1]Qiong Zhang, et al. Discovery of EGFR Selective 4,6-disubstituted Pyrimidines From a Combinatorial Kinase-Directed Heterocycle Library. J Am Chem Soc. 2006 Feb 22;128 (7) :2182-3.|[2]Zhiwei Yu, et al. Novel Irreversible EGFR Tyrosine Kinase Inhibitor 324674 Sensitizes Human Colon Carcinoma HT29 and SW480 Cells to Apoptosis by Blocking the EGFR Pathway. Biochem Biophys Res Commun. 2011 Aug 12;411 (4) :751-6.