Description
Dacomitinib-d10 (dihydrochloride) is the deuterium labeled Dacomitinib dihydrochloride. Dacomitinib (PF-00299804) dihydrochloride is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively[1].–20°C (Powder, protect from light)-Applications–Formula-C24H17D10Cl3FN5O2-Citation–References-[1]Engelman JA, et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to ZD1839. Cancer Res. 2007 Dec 15;67(24):11924-32.|[2]Kalous O, et al. Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to Anti-Human HER2 and GW572016. Mol Cancer Ther. 2012 Sep;11(9):1978-87.|[3]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. -CASNumber–MolecularWeight-552.92-Compound Purity-95.0-SMILES-O=C(/C=C/CN1C([2H])([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])C1([2H])[2H])NC2=CC3=C(C=C2OC)N=CN=C3NC4=CC=C(C(Cl)=C4)F.[H]Cl.[H]Cl-Research_Area-Cancer-Solubility-10 mM in DMSO-Target-Apoptosis;EGFR;Isotope-Labeled Compounds-Isoform–Pathway-Apoptosis;JAK/STAT Signaling;Others;Protein Tyrosine Kinase/RTK-MCE Product type-Isotope-Labeled Compounds
