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Erlotinib mesylate

  Cat. No.:  DC22486   Featured
Chemical Structure
248594-19-6
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Field of application
Erlotinib is an epidermal growth factor receptor inhibitor (EGFR inhibitor). Erlotinib HCl was approved. Erlotinib binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. For the signal to be transmitted, two EGFR molecules need to come together to form a homodimer. These then use the molecule of ATP to trans-phosphorylate each other on tyrosine residues, which generates phosphotyrosine residues, recruiting the phosphotyrosine-binding proteins to EGFR to assemble protein complexes that transduce signal cascades to the nucleus or activate other cellular biochemical processes. When erlotinib binds to EGFR, formation of phosphotyrosine residues in EGFR is not possible and the signal cascades are not initiated.
Cas No.: 248594-19-6
Chemical Name: Erlotinib Mesylate
Synonyms: Erlotinib (mesylate);CP-358774;NSC 718781;OSI-774;R 1415;N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine methanesulfonate
SMILES: CS(=O)(O)=O.COCCOC1=CC2=NC=NC(NC3=CC=CC(C#C)=C3)=C2C=C1OCCOC
Formula: C22H23N3O4.CH4O3S
M.Wt: 489.541
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Erlotinib (CP-358774;OSI-774;NSC 718781) is a potent, selective inhibitor of EGFR with IC50 of 2 nM; reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM; inhibits the proliferation of DiFi human colon tumor cells at submicromolar concentrations in cell culture and blocks cell cycle progression at the G1 phase; 100mg/kg completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice; orally active.Lung CancerApproved
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