| Icotinib HydrochlorideEGFR inhibitor,potent and specific |
Sample solution is provided at 25 µL, 10mM.
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Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| 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 | |||||
Icotinib Hydrochloride Dilution Calculator
Icotinib Hydrochloride Molarity Calculator
| 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 | N/A | ||
| Shipping Condition | N/A | ||
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.
