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Icotinib (Hydrochloride)

Product Name
Icotinib (Hydrochloride)
CAS No.
1204313-51-8
Chemical Name
Icotinib (Hydrochloride)
Synonyms
CS-1906;CS-1016;Icotinib HCl;Icotinib (Hydrochloride);Icotinib Hydrochloride (BPI-2009);Icotinib (Hydrochloride) impurity;N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine hydrochloride;N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine hydrochloride Icotinib (Hydrochloride)
CBNumber
CB22624183
Molecular Formula
C22H22ClN3O4
Formula Weight
427.89
MOL File
1204313-51-8.mol
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Icotinib (Hydrochloride) Property

storage temp. 
Store at -20°C
solubility 
Soluble in DMSO
form 
Powder
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0918
Product name
Icotinib(Hydrochloride)
Purity
99.99%
Packaging
5mg
Price
$70
Updated
2021/12/16
ChemScene
Product number
CS-0918
Product name
Icotinib(Hydrochloride)
Purity
99.99%
Packaging
10mg
Price
$100
Updated
2021/12/16
ApexBio Technology
Product number
A3482
Product name
IcotinibHydrochloride
Packaging
5mg
Price
$190
Updated
2021/12/16
ChemScene
Product number
CS-0918
Product name
Icotinib(Hydrochloride)
Purity
99.99%
Packaging
50mg
Price
$290
Updated
2021/12/16
Medical Isotopes, Inc.
Product number
110621
Product name
IcotinibHydrochloride
Packaging
300mg
Price
$690
Updated
2021/12/16
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Icotinib (Hydrochloride) Chemical Properties,Usage,Production

Clinical Use

Icotinib hydrochloride, developed by the Chinese pharmaceutical company Zhejiang Bata Pharma Inc., is a potent small molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor for the treatment of non-small cell lung cancer (NSCLC). It was first approved by the SFDA of China, and launched under the brand name Conmana in the middle of 2011, representing an important milestone for Chinese pharmaceutical research and development. As the third EGFR-TKI drug targeting NSCLS therapy, icotinib hydrochloride possesses a similar structure to gefitinib (Iressa, AstraZeneca) and erlotinib (Tarceva, OST & Roche). Interestingly, a randomized, double-blind phase III clinical study of icotinib versus gefitinib in 399 patients with advanced NSCLC demonstrated that icotinib provides similar efficacy to gefitinib, but with better tolerability in NSCLC patients previously treated with one or two chemotherapy agents.

Synthesis

Icotinib was prepared by a similar process approach to that of erlotinib. Beginning from commercially available 2,20-(ethylenedioxy)diethanol (162), bis-tosylation to 163, followed by bis-alkylation with commercially available catechol derivative 164 provided crown-4-ether 165 in 96% yield. Nitration of polyether 165 using concentrated nitric acid and concentrated sulfuric acid provided nitroarene 166 in 65% yield. Reduction of the nitroarene under catalytic hydrogenation conditions gave amine 167 in 85% yield. Condensation of the amine 167 with formamide in the presence of ammonium formate afforded quinazolinone 168 in 80% yield. The chlorination of 168 using POCl3 furnished quinazolyl chloride 169 in 77% yield. The treatment of chloride 169 with amine 170 followed by the HCl salt formation produced icotinib hydrochloride (XIV) in good yield.

target

EGFR

Icotinib (Hydrochloride) Preparation Products And Raw materials

Raw materials

Preparation Products

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Icotinib (Hydrochloride) Suppliers

AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
Fax
+1 (866) 333-9607
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info@adooq.com
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United States
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Target molecule Corp.
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857-239-0968
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service1@targetmol.com
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Musechem
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TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
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marketing@targetmol.com
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InvivoChem
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Fax
708-557-7486
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sales@invivochem.cn
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Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
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BOC Sciences
Tel
+1-631-485-4226
Fax
1-631-614-7828
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inquiry@bocsci.com
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Aladdin Scientific
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+1-+1(833)-552-7181
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ApexBio Technology
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Creative Enzymes
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info@creative-enzymes.com
Country
United States
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1204313-51-8, Icotinib (Hydrochloride)Related Search:


  • CS-1906
  • CS-1016
  • Icotinib Hydrochloride (BPI-2009)
  • Icotinib (Hydrochloride)
  • N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine hydrochloride
  • N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine hydrochloride Icotinib (Hydrochloride)
  • Icotinib HCl
  • Icotinib (Hydrochloride) impurity
  • 1204313-51-8
  • C22H21N3O4HCl
  • Inhibitors