Dacomitinib (PF299804) NEW

Factory Provide High Quality Dacomitinib Powder CAS 1110813-31-4

Introduction

Product Name : Dacomitinib (PF299804)

Other name:DacoMitinib (PF299804,PF-00299804);PF299804;DACOMITINIB;DacoMitinib (PF299804, PF299)

CAS No.:1110813-31-4

MF:C24H25ClFN5O2

Purity :99%

MW:469.94

Melting Point :184-187°C(dec.)(lit.)

Boiling Point :665.7±55.0 °C(Predicted)

Density :1.344g/cm3(Predicted)

Appearance: white powder

Storage :Sealed in dry,Sealed in dry,Room Temperature

Dacomitinib is an orally bioavailable, highly selective, second-generation small-molecule inhibitor of the pan-epidermal growth factor receptor (EGFR) family of tyrosine kinases (ErbB family) with potential antineoplastic activity. Dacomitinib specifically and irreversibly binds to and inhibits human EGFR subtypes, resulting in inhibition of proliferation and induction of apoptosis in EGFR-expressing tumor cells. EGFRs play major roles in tumor cell proliferation and tumor vascularization, and are often overexpressed or mutated in various tumor cell types.

Application 
Dacomitinib is a selective and irreversible inhibitor of EGFR. It is a drug candidate for the treatment of non-small cell lung carcinoma. It is current under the Phase III clinical trials. It also shows potential for the treatment of HER-2 amplified breast cancer cells lines that are resistant to trastuzumab and lapatinib. 
Biological activityDacomitibib (Dacomitinib, PF299804) is an effective and irreversible pan-ErbB inhibitor that is most effective in EGFR, with an IC50 of 6 nM. It is also highly effective in NSCLCs that carries EGFR or ERBB2 mutants (against Gefitinib) and EGFR T790M mutant. Phase 2.