Icotinib
Icotinib
- CAS:
- 610798-31-7
- MF:
- C22H21N3O4
- MW:
- 391.42
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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 Information
- Symbol(GHS)
GHS07
- Signal word
- Warning
- Hazard statements
- H302
- Precautionary statements
- P264-P270-P301+P312-P330-P501
- HS Code
- 29339900
Use
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.
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