Erlotinib-d4

Erlotinib-d4 (CP-358774-d4) is deuterium labeled Erlotinib. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer[1]. Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

[1130852-41-3]

Product Name Alternative

CP-358774-d4; NSC 718781-d4; OSI-774-d4

UNSPSC

12352005

Target

Autophagy; EGFR; Isotope-Labeled Compounds

Related Pathways

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

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

COCCOC(C(OCCOC)=C1)=CC2=C1C(NC3=C([2H])C(C#C)=C([2H])C([2H])=C3[2H])=NC=N2

Molecular Formula

C22H19D4N3O4

Molecular Weight

397.46

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[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]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, 57 (21), 4838-4848.|[4]Wada Y, et al. Epidermal growth factor receptor inhibition with erlotinib partially prevents cisplatin-induced nephrotoxicity in rats. PLoS One. 2014 Nov 12;9 (11) :e111728.