Selpercatinib-d3

Selpercatinib-d3 (LOXO-292-d3) is deuterium labeled Selpercatinib. Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC50 values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity[1][2].

2433775-55-2

LOXO-292-d3

12352005

Isotope-Labeled Compounds; RET

Others; Protein Tyrosine Kinase/RTK

Cancer-Kinase/protease

Cancer

N#CC1=C2C(C3=CN=C(N4CC5N(C(C5)C4)CC6=CN=C(OC([2H])([2H])[2H])C=C6)C=C3)=CC(OCC(C)(O)C)=CN2N=C1

C29H28D3N7O3

528.62

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Şentürk R, et, al. Quantitative bioanalytical assay for the selective RET inhibitors selpercatinib and pralsetinib in mouse plasma and tissue homogenates using liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2020 Jun 15;1147:122131.|[3]Steven W. Andrews, et al. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors. WO2018071447A1.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-W759629/

Isotope-Labeled Compounds

No Development Reported