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Icotinib (Hydrochloride)

(CAS: 1204313-51-8)

Suppliers of Icotinib (Hydrochloride)

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Active Biochem [email protected]; [email protected] 1-800-857-0985 (USA Toll Free#) USA

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Apexbio Technology LLC [email protected] +1-832-696-8203 USA

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BOC Sciences [email protected]bocsci.com 1-631-504-6093

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CHEMSCENE, LLC [email protected] 732-484-9848 USA

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DC Chemicals [email protected]; [email protected] +86-21-58447131 China

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MedChemexpress Co., Ltd. [email protected] 609-228-6898 USA

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Quality Control & MSDS Files: NP-HPLC HNMR MSDS

MedKoo Biosciences, Inc. [email protected] 919-279-0682 USA

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Shanghai Haoyuan Chemexpress Co., Ltd. [email protected] +86 (21) 5187-0955 / +86 (21) 5895-5995 China

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Target Molecule Corp. [email protected] (857) 239-0968 USA

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Background Information of Icotinib (Hydrochloride)

Icotinib Hcl(BPI-2009H) is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC(50) of 5 nM, including it's mutants of EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R). IC50 value: 5 nM Target: EGFR and EGFR mutants in vitro: Icotinib inhibits EGFR activity in a dose-dependent manner, with an IC50 value of 5 nM and complete inhibition at 62.5 nM.

Solubility of Icotinib (Hydrochloride)

Solubility Sources
DMSO MedChemexpress Co., Ltd.

Storage Condition of Icotinib (Hydrochloride)

Storage Condition Sources

MSDS Information

MSDS Sources
MedChemexpress Co., Ltd.

Quality Control and Spectral Data

QC Reports Sources
[NP-HPLC] [HNMR] MedChemexpress Co., Ltd.

Mechanism and Indications

Signaling Pathways JAK/STAT Signaling Protein Tyrosine Kinase/RTK
Target EGFR
Research Area Cancer
Indications Metastasis Metastatic non small cell lung cancer

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Icotinib (Hydrochloride) Zhejiang Beta Pharma Inc Metastasis 2013/6/30 2014/12/31 Phase 4 Clinical
Icotinib (Hydrochloride) Zhejiang Beta Pharma Inc Metastatic non small cell lung cancer 2012/10/31 2014/4/30 Phase 4 Clinical
Icotinib (Hydrochloride) Zhejiang Beta Pharma Inc Metastatic non small cell lung cancer 2012/8/31 2013/12/31 Phase 4 Clinical
Icotinib (Hydrochloride) Zhejiang Beta Pharma Inc Metastatic non small cell lung cancer 2012/7/31 2014/10/31 Phase 4 Clinical
Icotinib (Hydrochloride) Zhejiang Beta Pharma Inc Metastatic non small cell lung cancer 2011/9/30 2013/11/30 Phase 4 Clinical
Icotinib (Hydrochloride) - Launched

Chemical Information

M.Wt Formula CAS No. Synonyms
427.88 C22H22ClN3O4 1204313-51-8 BPI-2009H; N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine hydrochloride

Structure Information of Icotinib (Hydrochloride)

Smiles C#CC1=CC(NC2=C(C=C(OCCOCCOCCO3)C3=C4)C4=NC=N2)=CC=C1.[H]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

Related Products

Other Form Products of Icotinib (Hydrochloride)

Name CAS Formula Suppliers
Icotinib 610798-31-7 C22H21N3O4 9

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Chemical and Physical Properties

Appearance:White to off-white solid Melting point:
Boiling point: Flash Point:
Water Solubility: Solubility:
Density: Merck:
BRN: Refractive Index:
Vapour: EINECS:
Optical Rotation: alpha:


[1].Tan F, et al. Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies. Lung Cancer. 2012 May;76(2):177-82.
Icotinib, one of the leading compounds selected from our compound library, was found to be a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC(50) of 5 nM. When profiled with 88 kinases, Icotinib only showed meaningful inhibitory activity to EGFR and its mutants. Icotinib blocked EGFR-mediated intracellular tyrosine phosphorylation (IC(50)=45 nM) in the human epidermoid carcinoma A431 cell line and inhibits tumor cell proliferation. In vivo studies demonstrated that Icotinib exhibited potent dose-dependent antitumor effects in nude mice carrying a variety of human tumor-derived xenografts. The drug was well tolerated at doses up to 120 mg/kg/day in mice without mortality or significant body weight loss during the treatment. A head to head randomized, double blind phase III trial using Gefitinib as an active control for patients with advanced non-small cell lung cancer (NSCLC) was finished recently (Trial registration ID: NCT01040780). The data shows that Icotinib was non-inferior to Gefitinib in terms of median progression free survival (PFS) and safety superior favor to Icotinib compared to Gefitinib.

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