Lapatinib-d4

Names

[ CAS No. ]:
1184263-99-7

[ Name ]:
Lapatinib-d4

Biological Activity

[Description]:

Lapatinib-d4 (GW572016-d4) is the deuterium labeled Lapatinib (HY-50898). Lapatinib is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1][2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR
Signaling Pathways >> Apoptosis >> Ferroptosis
Signaling Pathways >> Autophagy >> Autophagy

[In Vitro]

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

[References]

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

[2]. Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94.  

Chemical & Physical Properties

[ Molecular Formula ]:
C29H22D4ClFN4O4S

[ Molecular Weight ]:
585.08

Related Compounds