Dacomitinib (PF299804,PF-00299804) 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.Dacomitinib (PF299804,PF-00299804) is a quinazalone-based irreversible pan-ERBB inhibitor structurally related to CI-1033. Dacomitinib (PF299804,PF-00299804) is a potent inhibitor of EGFR-activating mutations as well as the EGFR T790M resistance mutation both in vitro and in vivo. Additionally, Dacomitinib (PF299804,PF-00299804) is a highly effective inhibitor of both the wild-type ERBB2 and the gefitinib-resistant oncogenic ERBB2 mutation identified in lung cancers. Dacomitinib (PF299804,PF-00299804) 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, Dacomitinib (PF299804,PF-00299804) also effectively inhibited wild-type ERBB2. LCK and SRC were the only other kinases inhibited by Dacomitinib (PF299804,PF-00299804) 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. Dacomitinib (PF299804,PF-00299804) is active in E-sensitive and -resistant preclinical models. Dacomitinib (PF299804,PF-00299804) had clinical activity in phase I/II trials in EGFR TK inhibitor (TKI)-refractory NSCLC.Dacomitinib (PF299804,PF-00299804) is originally developed by Seoul National University Hospital and Pfizer. The phase II clinical trials for Dacomitinib (PF299804,PF-00299804) was performing in the treatment of advanced gastric cancer.

June 21, 2017

prudect name : Dacomitinib (PF299804,PF-00299804) 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.Dacomitinib (PF299804,PF-00299804) is a quinazalone-based irreversible pan-ERBB inhibitor structurally related to CI-1033. Dacomitinib (PF299804,PF-00299804) is a potent inhibitor of EGFR-activating mutations as well as the EGFR T790M resistance mutation both in vitro and in vivo. Additionally, Dacomitinib (PF299804,PF-00299804) is a highly effective inhibitor of both the wild-type ERBB2 and the gefitinib-resistant oncogenic ERBB2 mutation identified in lung cancers. Dacomitinib (PF299804,PF-00299804) 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, Dacomitinib (PF299804,PF-00299804) also effectively inhibited wild-type ERBB2. LCK and SRC were the only other kinases inhibited by Dacomitinib (PF299804,PF-00299804) 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. Dacomitinib (PF299804,PF-00299804) is active in E-sensitive and -resistant preclinical models. Dacomitinib (PF299804,PF-00299804) had clinical activity in phase I/II trials in EGFR TK inhibitor (TKI)-refractory NSCLC.Dacomitinib (PF299804,PF-00299804) is originally developed by Seoul National University Hospital and Pfizer. The phase II clinical trials for Dacomitinib (PF299804,PF-00299804) was performing in the treatment of advanced gastric cancer.
PF299804(Dacomitinib)

Synonyms: PF299804(Dacomitinib)CAS NO: 1110813-31-4Molecular Formula: C₂₄H₂₅ClFN₅O₂Molecular Weight: 469.94Purity: 98% minSolubility: In DMSOStorage: -20°C

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