PZ0330

Dacomitinib

≥98% (HPLC)

• Synonym(s): (2E)-N-[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide, PF-00299804, PF-00299804-03, PF-299
• Empirical Formula (Hill Notation): C₂₄H₂₅ClFN₅O₂
• CAS Number: 1110813-31-4
• Molecular Weight: 469.94
• UNSPSC Code: 41106609
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: room temp
• SMILES string: Fc1c(cc(cc1)Nc2ncnc3c2cc(c(c3)OC)NC(=O)\C=C\CN4CCCCC4)Cl
• InChI: 1S/C24H25ClFN5O2/c1-33-22-14-20-17(24(28-15-27-20)29-16-7-8-19(26)18(25)12-16)13-21(22)30-23(32)6-5-11-31-9-3-2-4-10-31/h5-8,12-15H,2-4,9-11H2,1H3,(H,30,32)(H,27,28,29)/b6-5+
• InChI key: LVXJQMNHJWSHET-AATRIKPKSA-N

Description

Biochem/physiol Actions

Dacomitinib (PF-00299804) is an irreversible EGFR inhibitor and antineoplastic. It is a potent inhibitor of HER-1 (EGFR), -2 and -4 tyrosine kinase with IC50s of 6.0, 45.7 and 73.7 nM respectively for EGFR, ERBB2 and ERBB4. Dacomitinib is believed to irreversibly inhibit erbB tyrosine kinase activity through binding at the ATP site and covalent modification of nucleophilic cysteine residues in the catalytic domains of erbB family members.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable