Lapatinib-d7 ditosylate

Modify Date: 2024-01-12 22:19:13

Lapatinib-d7 ditosylate Structure
Lapatinib-d7 ditosylate structure
Common Name Lapatinib-d7 ditosylate
CAS Number 1009307-24-7 Molecular Weight 753.25900
Density N/A Boiling Point N/A
Molecular Formula C36H34ClFN4O7S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Lapatinib-d7 ditosylate


Lapatinib-d7 (GW572016-d7) ditosylate is the deuterium labeled Lapatinib. Lapatinib (GW572016) 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].

 Names

Name N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[1,1,2,2-tetradeuterio-2-(trideuteriomethylsulfonyl)ethyl]amino]methyl]furan-2-yl]quinazolin-4-amine,4-methylbenzenesulfonic acid
Synonym More Synonyms

 Lapatinib-d7 ditosylate Biological Activity

Description Lapatinib-d7 (GW572016-d7) ditosylate is the deuterium labeled Lapatinib. Lapatinib (GW572016) 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
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;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 C36H34ClFN4O7S2
Molecular Weight 753.25900
Exact Mass 752.15400
PSA 177.48000
LogP 10.00630

 Synonyms

N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl-d7]amino]methyl]-2-furanyl]-4-quinazolinamine Bis(4-methylbenzenesulfonate) Ditosylate
Tykerb-d7 Ditosylate
Lapatinib-d7 Ditosylate