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IcotinibEGFR tyrosine kinase inhibitor

Icotinib

Catalog No. B1496
Size Price Stock Qty
5mg $190.00 In stock
10mg $260.00 In stock
50mg $780.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Icotinib

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Chemical Properties

Cas No. 610798-31-7 SDF Download SDF
Chemical Name N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine
Canonical SMILES [H]C1=C2OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC2=C([H])C3=NC([H])=NC(N([H])C4=C([H])C([H])=C([H])C(C#C[H])=C4[H])=C31
Formula C22H21N3O4 M.Wt 391.42
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Icotinib is a potent and specific EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor (IC50 = 5 nM) [1]

EGFR are family of receptor tyrosine kinase that is a transmembrane protein involved in the regulation of cell proliferation, motility and apoptosis. EGFR are expressed in various human cancer types, including breast, head & neck, NSCLC (non-small cell lung cancer) and ovarian caners. [1]

In human epidermoid carcinoma A431 cell line, Icotinib inhibited EGF-induced EGFR phosphorylation in a dose-dependent manner. Icotinib inhibited tyrosine phosphorylation of a variety of intracellular proteins. [1]

In different types of tumor xenograft mice models, Icotinib inhibited tumor growth in a dose-dependent manner without pronounced adverse effect in body weight loss and toxicity signs. In a randomized, double-blind, Gefitinib as control and multi-center phase III trial, Icotinib demonstrated efficacy on NSCLC in advanced stage. [1]

Reference:
[1] Tan F, Shen X, Wang D, Xie G, Zhang X, Ding L, Hu Y, He W, Wang Y, Wang Y.  Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies.  Lung Cancer. 2012 May;76(2):177-82.