PF299804 is a potent, orally available, irreversible tyrosine kinase HER 1 (EGFR), HER2 and HER4 inhibitor with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2 and ERBB4, respectively.PF299804 is a quinazalone-based irreversible pan-ERBB inhibitor structurally related to CI-1033. PF299804 is a potent inhibitor of EGFR-activating mutations as well as the EGFR T790M resistance mutation both in vitro and in vivo. Additionally, PF299804 is a highly effective inhibitor of both the wild-type ERBB2 and the gefitinib-resistant oncogenic ERBB2 mutation identified in lung cancers. PF299804 effectively inhibited the in vitro kinase activity of wild-type EGFR with similar efficacy as gefitinib, erlotinib, andCI-1033. In contrast to gefitinib and erlotinib, PF299804 also effectively inhibited wild-type ERBB2. LCK and SRC were the only other kinases inhibited by PF299804 although with >10 fold higher IC50 than against EGFR. PF299804 inhibited cellular EGFR and ERBB 2 with IC50 of 5.8 and 41 nM in NIH3T3/EGFR cell and NIH3T3/ERBB2 cell, respectively. PF299804 is active in E-sensitive and -resistant preclinical models. PF299804 had clinical activity in phase I/II trials in EGFR TK inhibitor (TKI)-refractory NSCLC. PF299804 is originally developed by Seoul National University Hospital and Pfizer. The phase II clinical trials for PF299804 was performing in the treatment of advanced gastric cancer.

June 21, 2017

prudect name : PF299804 is a potent, orally available, irreversible tyrosine kinase HER 1 (EGFR), HER2 and HER4 inhibitor with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2 and ERBB4, respectively.PF299804 is a quinazalone-based irreversible pan-ERBB inhibitor structurally related to CI-1033. PF299804 is a potent inhibitor of EGFR-activating mutations as well as the EGFR T790M resistance mutation both in vitro and in vivo. Additionally, PF299804 is a highly effective inhibitor of both the wild-type ERBB2 and the gefitinib-resistant oncogenic ERBB2 mutation identified in lung cancers. PF299804 effectively inhibited the in vitro kinase activity of wild-type EGFR with similar efficacy as gefitinib, erlotinib, andCI-1033. In contrast to gefitinib and erlotinib, PF299804 also effectively inhibited wild-type ERBB2. LCK and SRC were the only other kinases inhibited by PF299804 although with >10 fold higher IC50 than against EGFR. PF299804 inhibited cellular EGFR and ERBB 2 with IC50 of 5.8 and 41 nM in NIH3T3/EGFR cell and NIH3T3/ERBB2 cell, respectively. PF299804 is active in E-sensitive and -resistant preclinical models. PF299804 had clinical activity in phase I/II trials in EGFR TK inhibitor (TKI)-refractory NSCLC. PF299804 is originally developed by Seoul National University Hospital and Pfizer. The phase II clinical trials for PF299804 was performing in the treatment of advanced gastric cancer.
PF-00299804 dacomitinib

Synonyms: PF-00299804 dacomitinibCAS NO: 1042385-75-0Molecular Formula: C₂₄H₂₇ClFN₅O₃Molecular Weight: 469.17Purity: 98% minSolubility: In DMSOStorage: -20°C

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