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Icotinib

Icotinib Structure
CAS No.
610798-31-7
Chemical Name:
Icotinib
Synonyms
ConMana;N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine;otinib;CS-908;BP-1096;BPI-2009;Icotinib;Lcotinib;BPI-2009H;Icotinib BP-1096
CBNumber:
CB82616025
Molecular Formula:
C22H21N3O4
Molecular Weight:
391.42
MOL File:
610798-31-7.mol
MSDS File:
SDS
Modify Date:
2024/7/2 8:55:20

Icotinib Properties

Boiling point 581℃
Density 1.31
Flash point 305℃
storage temp. Store at -20°C
solubility insoluble in H2O; ≥129.6 mg/mL in DMSO; ≥14.13 mg/mL in EtOH with ultrasonic
form Powder
pka 5.32±0.20(Predicted)
color White to off-white

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P264-P270-P301+P312-P330-P501
HS Code  29339900
NFPA 704
0
2 0

Icotinib Chemical Properties,Uses,Production

Description

Icotinib is also known as ConMana. It is a highly selective, first-generation inhibitor of epidermal growth factor receptor tyrosine kinase (EGFR-TKI), whose mutation and overexpression is involved in many kinds of cancer. Icotinib is a quinazoline derivative that binds reversibly to the ATP binding site of the EGFR protein, being capable of blocking the signal transduction cascade. It is currently under investigation for its treatment efficacy on the EGFR+ Non-small cell lung cancer.

Uses

Icotinib is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with IC50 of 5 nM.

Indications

Icotinib (Conmana?, BetaPharma), an EGFR inhibitor, was approved by the China State FDA in 2011 for the treatment of NSCLC. Icotinib resembles erlotinib in possessing the N-(3-ethylnylphenyl) quinazolin-4-amine core scaffold of erlotinib that binds to the EGFR ATP pocket. An adjacent hydrophobic group was also retained while the solvent exposed two 2-methoxyethyoxysubstituents at the 6- and 7-positions of the quinazoline core were cyclized to afford the tetraoxacyclododecene moiety of icotinib. Efficacy and safety of icotinib as first-line therapy in patients has been evaluated for advanced NSCLC in recent clinical studies.

General Description

Class: receptor tyrosine kinase
Treatment: NSCLC
Oral bioavailability = 52%
Elimination half-life = 5.5 h

References

Tan, F., et al. "Icotinib (BPI-2009H), a novel EGFR tyrosine kinase inhibitor, displays potent efficacy in preclinical studies. " Lung Cancer76.2(2012):177-82.
Shi, Y., et al. "Icotinib versus gefitinib in previously treated advanced non-small-cell lung cancer (ICOGEN): a randomised, double-blind phase 3 non-inferiority trial." Lancet Oncology 14.10(2013):953-61.
Sun, Y., Y. Shi, and L. Zhang. "A randomized, double-blind phase III study of icotinib versus gefitinib in patients with advanced non-small cell lung cancer (NSCLC) previously treated with chemotherapy (ICOGEN)."Journal of Thoracic Oncology 29.15(2011):-.
https://en.wikipedia.org/wiki/Icotinib

Icotinib Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 111)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
A.J Chemicals 91-9810153283 New Delhi, India 6124 58 Inquiry
CLEARSYNTH LABS LTD. +91-22-45045900 Hyderabad, India 6351 58 Inquiry
Capot Chemical Co.,Ltd. 571-85586718 +8613336195806 China 29798 60 Inquiry
career henan chemical co +86-0371-86658258 +8613203830695 China 29901 58 Inquiry
BOC Sciences +1-631-485-4226 United States 19553 58 Inquiry
Chongqing Chemdad Co., Ltd +86-023-6139-8061 +86-86-13650506873 China 39916 58 Inquiry
Dideu Industries Group Limited +86-29-89586680 +86-15129568250 China 26368 58 Inquiry
Baoji Guokang Bio-Technology Co., Ltd. 0917-3909592 13892490616 China 9327 58 Inquiry
Zhejiang J&C Biological Technology Co.,Limited +1-2135480471 +1-2135480471 China 10522 58 Inquiry
InvivoChem +1-708-310-1919 +1-13798911105 United States 6393 58 Inquiry

Icotinib Spectrum

BPI-2009 BP-1096 BPI-2009H Lcotinib Icotinib [1,4,7,10]Tetraoxacyclododecino[2,3-g]quinazolin-4-amine, N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro- Icotinib int. N-1 N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin otinib Icotinib USP/EP/BP Icotinib(BPI-2009H) CS-908 Icotinib BP-1096 Icotinib, 98%, a potent EGFR inhibitor BPI-2009H;BPI-2009 Icotinib (BPI-2009) ConMana N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine Icotinib,apotentEGFRinhibitor 610798-31-7 610793-31-7 Inhibitors API