Erlotinib (mesylate)

Erlotinib mesylate (CP-358774 mesylate) inhibits purified EGFR kinase with an IC50 of 2 nM. Erlotinib (mesylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

[248594-19-6]

Product Name Alternative

CP-358774 (mesylate) ; NSC 718781 (mesylate) ; OSI-774 (mesylate)

UNSPSC

12352005

Target

Autophagy; EGFR

Type

Reference compound

Related Pathways

Autophagy; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/erlotinib-mesylate.html

Solubility

10 mM in DMSO

Smiles

CS(=O)(O)=O.COCCOC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCOC

Molecular Formula

C23H27N3O7S

Molecular Weight

489.54

References & Citations

[1]Moyer JD, et al. Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res. 1997 Nov 1;57 (21) :4838-48.|[2]Ali S, et al. Apoptosis-inducing effect of erlotinib is potentiated by 3,3'-diindolylmethane in vitro and in vivo using an orthotopic model of pancreatic cancer. Mol Cancer Ther, 2008, 7 (6), 1708-1719.|[3]Marchetti S, et al. Effect of the ATP-binding cassette drug transporters ABCB1, ABCG2, and ABCC2 on erlotinib hydrochloride (Tarceva) disposition in in vitro and in vivo pharmacokinetic studies employing Bcrp1-/-/Mdr1a/1b-/- (triple-knockout) and wild-type mice.Mol Cancer Ther. 2008 Aug;7 (8) :2280-7.|[4]Adachi K, et al. Effects of erlotinib on lung injury induced by intratracheal administration of bleomycin (BLM) in rats. J Toxicol Sci. 2010 Aug;35 (4) :503-14.