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Icotinib HydrochlorideEGFR inhibitor,potent and specific

Icotinib Hydrochloride

Catalog No. A3482
Size Price Stock Qty
5mg $238.00 In stock
10mg $342.00 In stock
50mg $998.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Icotinib Hydrochloride

Biological Activity

Description Icotinib Hydrochloride is a potent and specific inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinases with IC50 value of 5 nM.
Targets EGFR          
IC50 5 nM          

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Chemical Properties

Cas No. 1204313-51-8 SDF Download SDF
Synonyms BPI-2009H
Chemical Name N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine hydrochloride
Canonical SMILES Cl[H].[H]C1=C2C(N=C([H])N=C2N([H])C3=C([H])C([H])=C([H])C(C#C[H])=C3[H])=C([H])C4=C1OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])C([H])([H])O4
Formula C22H22ClN3O4 M.Wt 427.88
Solubility Soluble in DMSO 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 Hydrochloride is a potent and highly selective inhibitor of epidermal growth factor receptor tyrosine kinases (EGFR-TKI) with IC50 value of 5 nM.
EGFR is an oncogenic driver which is expressed on the cell surface of normal cells and cancer cells [1], and patients with somatic mutations, particularly an exon 19 deletion or exon 21 L858R mutation, within the tyrosine kinase domain have activating mutations that lead to unchecked cell proliferation.[2] Overexpression of EGFR caused inappropriate activation of the anti-apoptotic Ras signaling pathway, found in many different types of cancer.[3]
Icotinib is a quinazoline derivative that binds reversibly to the ATP binding site of the EGFR protein, preventing completion of the signal transduction cascade.[4] Icotinib inhibited the intracellular phosphorylation of tyrosine kinase(TK) associated with the epidermal growth factor receptor (EGFR).[5]
Icotinib is indicated for the treatment for EGFR mutation-positive, advanced or metastatic non-small cell lung cancer (NSCLC) as a second-line or third-line treatment, for patients who have failed at least one prior treatment with platinum-based chemotherapy.[6]
References:
1.A Douglas Laird,and Julie M Cherrington. Small molecule tyrosine kinase inhibitors: clinical development of anticancer agents. 2003, 12(1): 51-64.
2.Raymond E, Faivre S, Armand JP: Epidermal growth factor receptor tyrosine kinase as a target for anticancer therapy. Drugs. 2000;60 Suppl 1:15-23.
3.Sordella,R. "Gefitinib-Sensitizing EGFR Mutations in Lung Cancer Activate Anti-Apoptotic Pathways". Science ,2004, 305 (5687): 1163-1167.
4.Bulgaru AM. et al. Erlotinib (Tarceva): a promising drug targeting epidermal growth factor receptor tyrosine kinase. Expert Rev Anticancer Ther. 2003 Jun;3(3):269-79.
5.Dudek AZ.et al. Skin rash and bronchoalveolar histology correlates with clinical benefit in patients treated with gefitinib as a therapy for previously treated advanced or metastatic non-small cell lung cancer. Lung Cancer. 2006, 51(1):89-96.
6.C Delbaldo, S Faivre, E Raymond. Les inhibiteurs des récepteurs de l’Epidermal Growth Factor (EGF) Epidermal growth factor inhibitors. La Revue de Médecine Interne. 2003,24(6): 372–383.