Basic Information

• Product Name: Gefitinib

• CAS Number: 184475-35-2

• Molecular Formula: C22H24ClFN4O3

• Molecular Weight: 446.902 g/mol

• Appearance: White to beige powder

Physical Properties

• Density: Approximately 1.3±0.1 g/cm³

• Boiling Point: 586.8±50.0 °C at 760 mmHg

• Melting Point: 119-120 °C

• Flash Point: 308.7±30.1 °C

• Refractive Index: 1.621

• Solubility: Soluble in DMSO (89 mg/mL at 25°C), methanol (20 mg/mL), and ethanol (4 mg/mL at 25°C); sparingly soluble in water (<1 mg/mL at 25°C)

Chemical Properties

• Selective EGFR-TK Inhibitor: Gefitinib is a potent and selective inhibitor of the epidermal growth factor receptor tyrosine kinase (EGFR-TK). It binds competitively to the ATP-binding site of the EGFR, thereby inhibiting EGFR autophosphorylation and downstream signaling.

• Antitumor Activity: By inhibiting EGFR-TK, Gefitinib can block tumor growth, metastasis, and angiogenesis, and increase tumor cell apoptosis. It has been approved for the treatment of non-small cell lung cancer (NSCLC) that has progressed after prior chemotherapy.

Storage Conditions

• Store at room temperature in a cool, dry place, away from direct sunlight and moisture.

• Avoid mixing or transporting with toxic or hazardous materials.

Pharmacological Effects

• Inhibition of EGFR Signaling: Gefitinib specifically inhibits the activity of EGFR tyrosine kinase, thereby interfering with tumor cell proliferation, migration, and invasion.

• Enhancement of Chemotherapeutic Efficacy: It can enhance the efficacy of cytotoxic agents when used in combination.