|4-methyl Erlotinib EGFR inhibitor|
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||1346601-52-2||SDF||Download SDF|
|Solubility||≤0.25mg/ml in ethanol;25mg/ml in DMSO;50mg/ml in dimethyl formamide||Storage||Store at -20°C|
|Physical Appearance||A crystalline solid||Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For 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.|
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) .
The epidermal growth factor receptor (EGFR) autocrine pathway has been important for cancer development and progression, including cell proliferation, apoptosis, angiogenesis, and metastatic spread .
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 .
Erlotinib can prolong survival in patients with non–small-cell lung cancer after first-line or second-line chemotherapy .
 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).
 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.
 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.