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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

[183321-74-6]

Product Name Alternative

CP-358774; NSC 718781; OSI-774

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

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.html

Purity

99.99

Solubility

DMSO : 33.33 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

C#CC1=CC=CC(NC2=NC=NC3=C2C=C(C(OCCOC)=C3)OCCOC)=C1

Molecular Formula

C22H23N3O4

Molecular Weight

393.44

Precautions

H302, H315, H319, H335

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, 57 (21), 4838-4848.|[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]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

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

EGFR/ErbB1/HER1

Citation 01

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