Dacomitinib-d10 (dihydrochloride)

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].

Product Specifications

Product Name Alternative

PF-00299804-d10 (dihydrochloride) ; PF-299804-d10 (dihydrochloride)

UNSPSC

12352005

Target

Apoptosis; EGFR; Isotope-Labeled Compounds

Type

Isotope-Labeled Compounds

Related Pathways

Apoptosis; JAK/STAT Signaling; Others; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Purity

95.0

Solubility

10 mM in DMSO

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

Molecular Formula

C24H17D10Cl3FN5O2

Molecular Weight

552.92

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]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.|[3]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.