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Erlotinib-d4

CAT: 0804-HY-50896S2Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-50896S2Size:1 Each
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Description
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.
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.
Shipping Conditions
Room temperature
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported

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