Vandetanib-d6
Vandetanib-d6 is the deuterium labeled Vandetanib. 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) [1].
Product Specifications
CAS Number
1174683-49-8
Product Name Alternative
ZD6474-d6
UNSPSC
12352005
Hazard Statement
H302-H360-H373-H410
Target
Apoptosis; Autophagy; Isotope-Labeled Compounds; VEGFR
Type
Isotope-Labeled Compounds
Related Pathways
Apoptosis; Autophagy; Others; Protein Tyrosine Kinase/RTK
Field of Research
Cancer
Solubility
10 mM in DMSO
Smiles
FC1=CC(Br)=CC=C1NC2=NC=NC3=CC(OCC4CCN(CC4)C([2H])([2H])[2H])=C(C=C23)OC([2H])([2H])[2H]
Molecular Formula
C22H18D6BrFN4O2
Molecular Weight
481.39
Precautions
P260-P264-P270-P273-P280-P330-P391-P405-P501
References & Citations
[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[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]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.|[4]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.|[5]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.
Shipping Conditions
Room temperature
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported
Frequently Asked Questions
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