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4-methyl Erlotinib EGFR inhibitor

Catalog No.C4727
Size Price Stock Qty
1mg
$72.00
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5mg
$322.00
In stock
10mg
$572.00
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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

4-methyl Erlotinib

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Chemical Properties

Cas No. 1346601-52-2 SDF Download SDF
Chemical Name N-(3-ethynyl-4-methylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine
Canonical SMILES COCCOC(C(OCCOC)=C1)=CC2=C1C(NC3=CC(C#C)=C(C)C=C3)=NC=N2
Formula C23H25N3O4 M.Wt 407.5
Solubility Soluble in DMSO Storage Store at -20°C
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.

Background

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].

References:
[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.