Erlotinib mesylate

Short Summary : EGFR inhibitor

Category : Tyrosine Kinase|EGFR

Purity : 0.98

CAS Number : 248594-19-6

Formula : C23H27N3O7S

Molecular Weight : 489.54

SMILE : COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC.CS(=O)(=O)O

Solubility : 25℃: DMSO

Storage : Store at -20°C

Description : Erlotinib mesylate is an oral selective inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase withIC50 value of 20 nM 1,2.
Erlotinib is an inhibitor targeting EGFR, it has been approved by FDA for the treatment of non-small-cell lung cancer (NSCLC), colorectal cancer and head and neck cancer. Erlotinib can bind to the ATP-binding site of EGFR reversibly and inhibit the autophosphorylation completely. This inhibition results in a subsequent inhibition of the downstream signal transduction pathways and causes cell cycle arrest and angiogenesis suppression. Besides that, Erlotinib also showed inhibitory activities against HER1 and HER2 kinases with IC50 values of 20-30 nM and 2-3 M, respectively 1.
References:1. Iyer R, Bharthuar A. A review of erlotinib-an oral, selective epidermal growth factor receptor tyrosine kinase inhibitor. Expert opinion on pharmacotherapy, 2010, 11(2): 311-320.2. Philip P A, Mahoney M R, Allmer C, et al. Phase II study of Erlotinib (OSI-774) in patients with advanced hepatocellular cancer. Journal of Clinical Oncology, 2005, 23(27): 6657-6663.

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