Icotinib
- CAS NO.:610798-31-7
- Empirical Formula: C22H21N3O4
- Molecular Weight: 391.42
- MDL number: MFCD22124501
- EINECS: 1592732-453-0
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:55:20
What is Icotinib?
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.
The Uses of Icotinib
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
Properties of Icotinib
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 information for Icotinib
Computed Descriptors for Icotinib
New Products
Tubulysin C Tubulysin B Tubulysin M Tubulysin E CYCLOBUTYLAMINE HYDROCHLORIDE Methyl (R)-1-Boc-4,4-difluoropyrrolidine-2-carboxylate tetrahydro-4-methyl-2H-pyran 2-(azetidin-3-ylidene)acetonitrile (hydrochloride) 3-METHYLAZETIDIN-3-OL HYDROCHLORIDE 3-N-BOC-(S)-AMINO BUTYRONITRILE 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol Fuel shell Calcium Sodium Phosphosilicate IH (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine Imeglimin Hydrochloride IH 1-(2,3-Dihydro- benzofuran-5-yl) -ethanone 3-(S)-(+)- (1-Cyano-1,1- diphenylmethyl)- 1-tosylpyrrolidine Latanoprostene Bunod Lubiprostone Magnesium Trisilicate Flame Retardant Zinc Borate 1H-Imidazole-4-carbonitrile 7-Methoxyquinoline-4-carboxylic acidRelated products of tetrahydrofuran
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