Toceranib-d8

Product Specifications

UNSPSC Description

Toceranib-d8 is the deuterium labeled Toceranib. Toceranib (SU11654) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib (SU11654) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors[1][2].

Target Antigen

c-Kit; Isotope-Labeled Compounds; PDGFR; VEGFR

Type

Isotope-Labeled Compounds

Related Pathways

Others;Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Solubility

10 mM in DMSO

Smiles

C(=C1C=2C(NC1=O)=CC=C(F)C2)C3=C(C)C(C(NCCN4C(C(C(C4([2H])[2H])([2H])[2H])([2H])[2H])([2H])[2H])=O)=C(C)N3

Molecular Weight

404.51

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.|[2]London CA, et al. Phase I dose-escalating study of SU11654, a small molecule receptor tyrosine kinase inhibitor, in dogs with spontaneous malignancies. Clin Cancer Res. 2003 Jul;9(7):2755-68.|[3]Halsey CH, et al. Development of an in vitro model of acquired resistance to toceranib phosphate (Palladia?) in canine mast cell tumor. BMC Vet Res. 2014 May 6;10:105.|[4]Mitchell L, et al. Clinical and immunomodulatory effects of toceranib combined with low-dose cyclophosphamide in dogs with cancer. J Vet Intern Med. 2012 Mar-Apr;26(2):355-62.