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4-methyl Erlotinib

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EGFR inhibitor
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4-methyl Erlotinib is an analog of erlotinib by the addition of a methyl group at the four position of the phenyl group. Erlotinib is a tyrosine kinase inhibitor which acts on the epidermal growth factor receptor (EGFR) [1].

The epidermal growth factor receptor (EGFR) autocrine pathway has been important for cancer development and progression, including cell proliferation, apoptosis, angiogenesis, and metastatic spread [2].

Erlotinib inhibits EGFR-associated kinase activity by binding to the EGF-activated receptor, with the phenyl group at one end sequestered in a hydrophobic pocket of the kinase domain and the ether linkages at the opposite end projecting into solvent [1].

Erlotinib can prolong survival in patients with non–small-cell lung cancer after first-line or second-line chemotherapy [3].

[1] Stamos, J. ,Sliwkowski, M.X. and Eigenbrot, C. Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor. The Journal of Biological Chemisty 277(48), 46265-46272 (2002).
[2] Ciardiello F, Tortora G.  A novel approach in the treatment of cancer: targeting the epidermal growth factor receptor[J]. Clinical Cancer Research, 2001, 7(10): 2958-2970.
[3] Shepherd F A, Rodrigues Pereira J, Ciuleanu T, et al.  Erlotinib in previously treated non–small-cell lung cancer[J]. New England Journal of Medicine, 2005, 353(2): 123-132.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
Cas No.1346601-52-2
Solubility≤0.25mg/ml in ethanol;25mg/ml in DMSO;50mg/ml in dimethyl formamide
Chemical NameN-(3-ethynyl-4-methylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine
SDFDownload SDF
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

4-methyl Erlotinib