Dacomitinib

Research use only, not for human use.

Dacomitinib (PF-00299804, PF-299804) is a potent, irreversible, orally active pan-ErbB receptor tyrosine kinase inhibitor with IC50 of 6, 45.7 and 73.7 for EGFR, ERBB2 and ERBB4, respectively.

Dacomitinib (PF-00299804, PF-299804) is a potent, irreversible, orally active pan-ErbB receptor tyrosine kinase inhibitor with IC50 of 6, 45.7 and 73.7 for EGFR, ERBB2 and ERBB4, respectively; irreversibly inhibits erbB tyrosine kinase activity through binding at the ATP site and covalent modification of nucleophilic cysteine residues in the catalytic domains of erbB family members inhibits erbB1 autophosphorylation in the A431 human squamous cell carcinoma line with IC50 of 15.1 nM; causes significant antitumor activity, including marked tumor regressions in a variety of human tumor xenograft models that express and/or overexpress erbB family members or contain the double mutation (L858R/T790M) in EGFR associated with resistance to gefitinib and erlotinib.Lung Cancer Phase 3 Clinical

PF-00299804;PF-299804;PF 299804;PF 00299804

Angiogenesis

EGFR

EGFR;HER2/ErbB2

Cancer

Lung Cancer

1110813-31-4

469.90

C24H25ClFN5O2

>98% (HPLC)

DMSO: ≥ 50 mg/mL (Need ultrasonic)

COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)NC(=O)/C=C/CN4CCCCC4

2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-, (2E)-

(-20℃)

With Ice Pack

≥ 2 years