Toceranib-d8

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].

Product Specifications

CAS Number

[1795134-78-9]

UNSPSC

12352005

Hazard Statement

H315, H319

Target

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

Purity

99.08

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 Formula

C22H17D8FN4O2

Molecular Weight

404.51

Precautions

H315, H319

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.