Vandetanib-13C6

Vandetanib-13C6 is a 13C labeled Vandetanib (HY-10260) [1]. Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM) . Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM) [2].

Product Specifications

CAS Number

[1261397-03-8]

Product Name Alternative

ZD6474-13C6

UNSPSC

12352005

Target

Apoptosis; Autophagy; Isotope-Labeled Compounds; VEGFR

Type

Isotope-Labeled Compounds

Related Pathways

Apoptosis; Autophagy; Others; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/vandetanib-13c6.html

Smiles

CN(CC1)CCC1COC(C(OC)=C2)=CC3=C2C(N[13C]4=[13C]([13CH]=[13C]([13CH]=[13CH]4)Br)F)=NC=N3

Molecular Formula

C16 13C6H24BrFN4O2

Molecular Weight

481.31

References & Citations

[1]Takeda H, et al. Vandetanib is effective in EGFR-mutant lung cancer cells with PTEN deficiency. Exp Cell Res. 2013 Feb 15;319 (4) :417-23.|[2]Wedge SR, et al. ZD6474 inhibits vascular endothelial growth factor signaling, angiogenesis, and tumor growth following oral administration. Cancer Res. 2002 Aug 15;62 (16) :4645-55.|[3]Inoue K, et al. Vandetanib, an inhibitor of VEGF receptor-2 and EGF receptor, suppresses tumor development and improves prognosis of liver cancer in mice. Clin Cancer Res. 2012 Jul 15;18 (14) :3924-33.|[4]Hegedus C, et al. Interaction of the EGFR inhibitors gefitinib, vandetanib, pelitinib and neratinib with the ABCG2 multidrug transporter: implications for the emergence and reversal of cancer drug resistance. Biochem Pharmacol. 2012 Aug 1;84 (3) :260-7.|[5]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.