Product Name: PF-06459988

Request PF-06459988

CAT#: A-6004


  Synonym:PF-06459988,

PF-06459988 Chemical Structure PF-06459988 chemical structure


IUPAC/Chemical name: 1-[(3R,4R)-3-[[[5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]oxy]methyl]-4-methoxy-1-pyrrolidinyl]-2-propen-1-one


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Biological Activity
An orally available, small molecule, third-generation, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant (EGFRm) forms with potential antineoplastic activity. EGFR inhibitor PF-06459988 specifically binds to and inhibits mutant forms of EGFR, including the secondary acquired resistance mutation T790M, which prevents EGFR-mediated signaling and leads to cell death in EGFRm-expressing tumor cells. Compared to some other EGFR inhibitors, PF-06459988 may have therapeutic benefits in tumors with T790M-mediated drug resistance. This agent shows minimal activity against wild-type EGFR (WT EGFR), and does not cause dose-limiting toxicities that are seen with the use of non-selective EGFR inhibitors, which also inhibit WT EGFR. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.
Technical Data
M.Wt:      431.88
Formula:     C19H22ClN7O3
CAS#: 1428774-45-1
Purity: >99% by HPLC
Storage Conditions: 0ºC to 4 ºC for short term or -20ºC for 3 years.

Reference