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Icotinib

Chemical Structure : Icotinib

CAS No.: 610798-31-7

Icotinib (BPI-2009, BPI 2009)

Catalog No.: PC-22087Not For Human Use, Lab Use Only.

Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with IC50 of 5 nM, also inhibits mutant EGFRL858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with IC50 of 5 nM, also inhibits mutant EGFRL858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q.
Icotinib only shows meaningful inhibitory activity to EGFR and its mutants against a panel of 88 kinases.
Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation (IC(50)=45 nM) in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation.
Icotinib exhibits potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts.

Physicochemical Properties

M.Wt 391.43
Formula C22H21N3O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine

References

1. Tan F, et al. Lung Cancer. 2012 May;76(2):177-82.

2. Yang G, et al. Oncol Rep. 2012 Jun;27(6):2066-72.

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