Buy Osimertinib Mesylate(AZD9291) best price /factory CAS NO.1421373-66-1

Buy Osimertinib Mesylate(AZD9291) best price /factory

Osimertinib is active against exon 19 deletions, exon 21 mutations, and also the exon 20 T790M mutations. It is preferentially selective for mutated EGFR, and therefore toxicity at therapeutic doses is lower than for first- and second-generation agents. Notably, osimertinib is able to cross the blood-brain barrier, making it active against disease in the CNS.

AZD9291 is a potent, selective, and irreversible, third generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). It inhibits EGFR phosphorylation in EGFR-bearing cells harboring sensitizing EGFR mutants with mean IC?? values ranging from 13 to 54 nM. It also potently inhibits phosphorylation of EGFR in T790M+ mutant cell lines. AZD-9291 displays profound and sustained tumor regression in EGFR-mutant tumor xenograft and transgenic models. 

The collection of ibrutinib (Imbruvica(R), Pharmacyclics Inc.), afatinib, and osimertinib represents the small, yet expanding, group of covalent SMKIs. Ibrutinib is a non-receptor Bruton’s tyrosine kinase inhibitor approved for the treatment of relapsed chronic lymphocytic leukemia. Afatinib, approved for NSCLC in 2013 and squamous NSCLC in 2016, is a second-generation irreversible EGFR inhibitor that targets wild-type EGFR, the mutant T790M EGFR, and HER2. Osimertinib (AZD9291), which was approved by FDA in November 2015, is a third-generation irreversible EGFR inhibitor that selectively targets the mutant T790M EGFR. Rociletinib, which shares a high degree of structural similarity with that of osimertinib, is a promising covalent EGFR inhibitor developed by Clovis Oncology aimed for the treatment of patients with EGFR T790M-mutated NSCLC, until the company terminated its development in May 2016 following a negative vote fromthe FDA’sOncologic Drugs Advisory Committee.