610798-31-7 Usage
Description
Icotinib, also known as ConMana, is a highly selective, first-generation inhibitor of epidermal growth factor receptor tyrosine kinase (EGFR-TKI). It is a quinazoline derivative that binds reversibly to the ATP binding site of the EGFR protein, effectively blocking the signal transduction cascade. Icotinib's action is particularly relevant due to the involvement of EGFR mutations and overexpression in various types of cancer.
Uses
Used in Pharmaceutical Industry:
Icotinib is used as an anticancer agent for targeting EGFR mutations associated with various types of cancer. Its application is primarily focused on non-small cell lung cancer (NSCLC), where it has shown potential in treating EGFR+ tumors by inhibiting the EGFR tyrosine kinase activity.
Used in Cancer Research:
Icotinib is utilized in the research and development of targeted cancer therapies. It is under investigation for its treatment efficacy on cancers with EGFR mutations, including non-small cell lung cancer. Icotinib's high specificity and potency make it a valuable tool in understanding the role of EGFR in cancer progression and developing new therapeutic strategies.
Used in Drug Development:
As a potent and specific EGFR tyrosine kinase inhibitor (TKI) with an IC50 of 5 nM, Icotinib serves as a starting point for the development of new, more effective, and less toxic treatments for EGFR-related cancers. Its properties guide the design and synthesis of next-generation EGFR inhibitors with improved pharmacokinetics, selectivity, and reduced side effects.
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.
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
Check Digit Verification of cas no
The CAS Registry Mumber 610798-31-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 6,1,0,7,9 and 8 respectively; the second part has 2 digits, 3 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 610798-31:
(8*6)+(7*1)+(6*0)+(5*7)+(4*9)+(3*8)+(2*3)+(1*1)=157
157 % 10 = 7
So 610798-31-7 is a valid CAS Registry Number.
610798-31-7Relevant articles and documents
Design, synthesis and antitumor activity of icotinib derivatives
Mao, Longfei,Sun, Ge,Zhao, Jie,Xu, Guiqing,Yuan, Miaomiao,Li, Yue-Ming
, (2020)
EGFR-TK pathway is of high importance for the treatment of non-small-cell lung cancers (NSCLC), and it will be challenging to develop anti-tumor drugs that could inhibit both EGFR wild-type and mutant tumor cells. Here, a series of icotinib derivatives containing 1,2,3-triazole moiety were designed and synthesized through copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) reactions. Preliminary CCK-8 assay showed that the prepared icotinib-1,2,3-triazole compounds such as a7 or a12 demonstrated potent in vitro antitumor activity against the NSCLC cells expressing both wild type EGFR and mutational EGFR. Further, the mechanism of action for compounds a7 and a12 induced NSCLC cells death was also detailed, and the results suggested a possible induced NSCLC cells death via inducing mitochondrial apoptosis and arresting cell cycle. Remarkably, the inhibition of EGFR by these icotinib derivatives was also studied. The results showed that compound a12 was a potent inhibitor for EGFR with IC50 value of 1.49 μM. Combining these results, an EGFR inhibitor a12 represents a promising new anti-NSCLC candidate that could induce apoptosis and arrest cell cycle.
Quinolinamine compound with IDO1 inhibition function and preparation method thereof
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Paragraph 0044-0046, (2020/11/23)
The invention discloses a quinolinamine compound with an IDO1 inhibition function and a preparation method of the quinolinamine compound, and belongs to the technical field of medicine synthesis. According to the technical scheme, triethylene glycol is us
POLYMORPH FORMS OF ICOTINIB MALEATE AND USES THEREOF
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Page/Page column 10; 11, (2015/01/09)
Provided are Icotinib maleate(the compound of Formula I) and polymorph forms thereof, and methods of preparing and using them.
