Dacomitinib, Free Base (PF299, PF299804, PF00299804, CAS 1110813-31-4), >99%

LC Laboratories' Product Number D-3700 - Dacomitinib, Free Base (PF299, PF299804, PF00299804, CAS 1110813-31-4), >99% - for research use only. Dacomitinib, also known as PF-00299804, is a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor. It irreversibly blocked erbB1 autophosphorylation in A431 human squamous carcinoma cells with an IC50 of 15.1 nM. It had significant antitumor activity in vivo, including marked tumor regressions in a variety of human tumor xenograft models that express and/or overexpress erbB family members or contain the double mutation (L858R/T790M) in erbB1 (EGFR) associated with resistance to gefitinib and erlotinib. A phase 2 clinical trial demonstrated that dacomitinib had clinical activity in recurrent/metastatic squamous-cell carcinoma of the head and neck (RM-SCCHN). Its toxicity was generally manageable with dose adjustments and interruptions. A phase 2 clinical trial demonstrated that dacomitinib significantly improved progression-free survival (PFS) versus erlotinib with acceptable toxicity in patients with advanced non-small-cell lung cancer. PFS benefit was shown in most clinical and molecular subsets, notably KRAS wild-type/EGFR any status, KRAS wild-type/EGFR wild-type, and EGFR mutants. Related CAS numbers: 1042385-75-0 for the hydrate (1:1).

• Supplier: LC Laboratories
• Product #: D-3700
• Sku #: D-3700_50mg