Gefitinib-d3

Gefitinib-d3 (ZD1839-d3) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].

1173976-40-3

12352005

Autophagy; EGFR; Isotope-Labeled Compounds

Isotope-Labeled Compounds

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

Cancer-Kinase/protease

Cancer

10 mM in DMSO

N(C=1C2=C(C=C(OC([2H])([2H])[2H])C(OCCCN3CCOCC3)=C2)N=CN1)C4=CC(Cl)=C(F)C=C4

C22H21D3ClFN4O3

449.92

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Pedersen MW, et al. Differential response to gefitinib of cells expressing normal EGFR and the mutant EGFRvIII. Br J Cancer. 2005 Oct 17;93 (8) :915-23.|[3]Moasser MM, et al. The tyrosine kinase inhibitor ZD1839 inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res. 2001 Oct 1;61 (19) :7184-8.|[4]Morgillo F, et al. Synergistic effects of 1,1-Dimethylbiguanide treatment in combination with gefitinib, a selective EGFR tyrosine kinase inhibitor, in LKB1 wild-type NSCLC cell lines. Clin Cancer Res. 2013 Jul 1;19 (13) :3508-19.|[5]Miyake K, et al. Epidermal growth factor receptor-tyrosine kinase inhibitor (gefitinib) augments pneumonitis, but attenuates lung fibrosis in response to radiation injury in rats. J Med Invest. 2012;59 (1-2) :174-85.|[6]Noh CK, et al. Simultaneous quantification of volitinib and gefitinib in rat plasma by HPLC-MS/MS for application to a pharmacokinetic study in rats. J Sep Sci. 2017 Jul 27.|[7]Dhar D, et al. Liver Cancer Initiation Requires p53 Inhibition by CD44-Enhanced Growth Factor Signaling. Cancer Cell. 2018 Jun 11;33 (6) :1061-1077.e6.|[8]Wakeling AE, et al. ZD1839: an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res. 2002 Oct 15;62 (20) :5749-54.

Room temperature

Isotope-Labeled Compounds