Icotinib hydrochloride

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Icotinib hydrochloride
Category Enzyme inhibitors
Catalog number BBF-04036
CAS 1204313-51-8
Molecular Weight 427.88
Molecular Formula C22H22ClN3O4
Purity >98%

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BBF-04036 300 mg $299 In stock

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Description

Icotinib Hydrochloride is a quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), which is upregulated in a variety of cancer cell types. Icotinib supresses the cancer cell proliferation via EGFR tyrosine kinase inhibition.

Specification

Related CAS 610798-31-7 (free base)
Synonyms Icotinib HCl; BPI-2009; BPI 2009; BPI2009
Storage Store at -20°C
IUPAC Name N-(3-ethynylphenyl)-2,5,8,11-tetraoxa-15,17-diazatricyclo[10.8.0.014,19]icosa-1(12),13,15,17,19-pentaen-18-amine;hydrochloride
Canonical SMILES C#CC1=CC(=CC=C1)NC2=NC=NC3=CC4=C(C=C32)OCCOCCOCCO4.Cl
InChI InChI=1S/C22H21N3O4.ClH/c1-2-16-4-3-5-17(12-16)25-22-18-13-20-21(14-19(18)23-15-24-22)29-11-9-27-7-6-26-8-10-28-20;/h1,3-5,12-15H,6-11H2,(H,23,24,25);1H
InChI Key PNNGXMJMUUJHAV-UHFFFAOYSA-N

Properties

Antibiotic Activity Spectrum neoplastics (Tumor)
Solubility Soluble in DMSO

Reference Reading

1.Phase I study of icotinib, an EGFR tyrosine kinase inhibitor combined with IMRT in nasopharyngeal carcinoma.
Hu W1, Wang W2, Yang P3, Zhou C2, Yang W2, Wu B4, Lu H5, Yang H2. Int J Clin Exp Med. 2015 Sep 15;8(9):15675-83. eCollection 2015.
BACKGROUND: Epidermal growth factor receptor (EGFR) is a new target for nasopharyngeal carcinoma (NPC) therapy. This prospective phase I study sought to determine the safety and recommended phase II dose of icotinib, a novel highly selective oral EGFR tyrosine kinase inhibitor, in combination with intensity-modulated radiotherapy (IMRT) in patients with NPC.
2.Personalized biomarkers to monitor disease progression in advanced non-small-cell lung cancer patients treated with icotinib.
Song G1, Liu Y1, Wang Y1, Ren G2, Guo S1, Ren J1, Zhang L2, Li Z3. Clin Chim Acta. 2015 Feb 2;440:44-8. doi: 10.1016/j.cca.2014.11.010. Epub 2014 Nov 15.
BACKGROUND: Disease-specific humoral immune response-related protein complexes in blood are associated with disease progression.
3.Icotinib hydrochloride enhances the effect of radiotherapy by affecting DNA repair in colorectal cancer cells.
Ma H1, Bi J1, Liu T1, Ke Y1, Zhang S1, Zhang T1. Oncol Rep. 2015 Mar;33(3):1161-70. doi: 10.3892/or.2014.3699. Epub 2014 Dec 30.
The aim of the present study was to explore the efficacy and mechanism of the radiosensitisation of icotinib hydrochloride (IH), a novel oral epidermal growth factor receptor-tyrosine kinase activity inhibitor, by evaluating the changes in tumour cell double-strand breaks (DSBs) repair, cell cycle and apoptosis following a combination of IH and radiotherapy (RT) in human colorectal adenocarcinoma cell lines. The HT29 and HCT116 human CRC cell lines were treated with IH and/or radiation. Effects on cell viability and cell cycle progression were measured by MTT, a clonogenic survival assay, and flow cytometry. Immunofluorescent staining and western blot analysis were applied to detect the expression of γ-H2AX and 53BP1 in the different treatment groups. Finally, the in vivo effect on the growth of CRC xenografts was assessed in athymic nude mice. IH inhibited the proliferation and enhanced the radiosensitivity in HT29 and HCT116 CRC cells lines.

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