Irreversible Inhibitor Dacomitinib CAS: 1110813-31-4 White Powder

Superiority

Zhongshan Latterson Biotechnology Co., Ltd., is a comprehensive pharmaceutical enterprise, which specialized in bio-pharmaceutical technology over 7 years. The company is located in Zhongshan City, Guangdong Province , China.
Our factory covers an area of 33500 square meters, with clean environment and nice layout. There are several large or medium workshops and QA and research center with advanced equipment. At present, our main products are Anabolic Steroid series, Peptide series, Local Anesthetic series. Our products reach the advanced standard of domestic market, many of which reach the international standard, certificates contain: KOSHER , ISO 9001:2008 , GMP , SGS.

Basic Information:

Product Name: Dacomitinib
Synonyms: Dacomitinib;PF-00299804-03;PF-00299804;DacoMitinib (PF-00299804);DacoMitinib,PF299804;DacoMitinib (PF299804,PF-00299804);DacoMitinib (PF299804, PF299);(2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide Dacomitinib (PF299804, PF299)
CAS: 1110813-31-4
MF: C24H25ClFN5O2
MW: 469.9390032
density: 1.344

Description:

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 activity:

Dacomitibib (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. Dacomitinib is taken orally once-daily. It is an irreversible inhibitor of HER-1 (EGFR), HER-2 and HER-4 tyrosine kinases. Dacomitinib targets multiple receptors of the HER pathway, whereas currently marketed HER-1 (EGFR) inhibitors for non-small cell lung cancer (NSCLC) target only one receptor in this pathway,developed by Pfizer.
Clinical Study Dacomitinib has advanced to several Phase III clinical trials. The results of the first trials were disappointing, with a failure to meet the study goals, Additional Phase III trials are ongoing. Clinical evaluation of dacomitinib is ongoing in a number of clinical trials in patients with advanced NSCLC across lines of therapies and a range of histologies and molecular subtypes, such as EGFR and KRAS status.
Additionally, there is an ongoing clinical trial evaluating dacomitinib in recurrent and/or metastatic (RM) squamous cell carcinoma of the head and neck (SCCHN).

Uses:

PF299804 is a potent, irreversible pan-ErbB inhibitor against ErbB1, ErbB2 and ErbB4 with IC50 of 6 nM, 45.7 nM and 73.7 nM, respectively.