Pelitinib-d6

Modify Date: 2024-01-31 13:30:24

Pelitinib-d6 Structure
Pelitinib-d6 structure
Common Name Pelitinib-d6
CAS Number 1325223-34-4 Molecular Weight 473.96
Density N/A Boiling Point N/A
Molecular Formula C24H17D6ClFN5O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Pelitinib-d6


Pelitinib-d6 (EKB-569-d6) is the deuterium labeled Pelitinib. Pelitinib (EKB-569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively[1][2].

 Names

Name Pelitinib-d6

 Pelitinib-d6 Biological Activity

Description Pelitinib-d6 (EKB-569-d6) is the deuterium labeled Pelitinib. Pelitinib (EKB-569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 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]. Torrance CJ, et al. Combinatorial chemoprevention of intestinal neoplasia. Nat Med. 2000 Sep;6(9):1024-8.

[3]. Nunes M, et al. Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes. Mol Cancer Ther. 2004 Jan;3(1):21-7.

 Chemical & Physical Properties

Molecular Formula C24H17D6ClFN5O2
Molecular Weight 473.96