Basic Information

• Product Name: Dacomitinib

• CAS Number: 1110813-31-4

• Molecular Formula: C24H25ClFN5O2

• Molecular Weight: 469.94

Physical and Chemical Properties

• Appearance: White to pale yellow solid

• Melting Point: 184-187°C

• Boiling Point: 665.7±55.0°C (predicted)

• Density: 1.344

• Solubility: Soluble in DMSO (slightly), methanol (slightly, with heating)

• pKa: 12.05±0.43 (predicted)

Biological Activity and Pharmacological Effects

• Mechanism of Action: Dacomitinib is a specific, irreversible inhibitor of the ERBB family kinases, with IC50 values of 6 nM, 45.7 nM, and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively. It inhibits both wild-type EGFR and EGFR mutants (such as T790M) and demonstrates activity in NSCLC cell lines that are sensitive and resistant to gefitinib.

• Inhibitory Effect: By irreversibly inhibiting ERBB tyrosine kinase activity, Dacomitinib inhibits cell growth and induces apoptosis. It has shown significant inhibitory effects on NSCLC in vitro and in vivo studies.