4-methyl Erlotinib
Catalogue Number: C4727-APE
| Manufacturer: | Apexbio |
| Molecular Formula: | C23H25N3O4 |
| Physical state: | A crystalline solid |
| Type: | Kinase Inhibitors |
| Shipping Condition: | Blue Ice |
| Unit(s): | 1 mg, 10 mg, 5 mg |
Description
Description: 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.
Additional Text
Storage Note
Store at -20°C
Solubility
≤0.25mg/ml in ethanol;25mg/ml in DMSO;50mg/ml in dimethyl formamide
Smile String
COCCOC(C(OCCOC)=C1)=CC2=C1C(NC3=CC(C#C)=C(C)C=C3)=NC=N2
C4727 CofA
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