Vandetanib-¹³C₆

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].
Vandetanib inhibits VEGFR3 and EGFR with IC₅₀ of 110 nM and 500 nM, respectively. Vandetanib is not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC₅₀ of 1.1-3.6 μM, while almost has no activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC₅₀ above 10 μM. Vandetanib inhibits VEGF-, EGF- and bFGF-stimulated HUVEC proliferation with IC₅₀ of 60 nM, 170 nM and 800 nM, with no effect on basal endothelial cell growth. Vandetanib inhibits tumor cell growth with IC₅₀ of 2.7 μM (A549) to 13.5 μM (Calu-6)^[2]. Odanacatib is a weak inhibitor of antigen presentation, measured in a mouse B cell line (IC₅₀=1.5±0.4 μM), compared to the Cat S inhibitor LHVS (IC₅₀=0.001 μM) in the same assay. Odanacatib also shows weak inhibition of the processing of the MHC II invariant chain protein Iip10 in mouse splenocytes compared to LHVS (minimum inhibitory concentration 1-10 μM versus 0.01 μM, respectively)^[3]. Vandetanib suppresses phosphorylation of VEGFR-2 in HUVECs and EGFR in hepatoma cells and inhibits cell proliferation^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.