Toceranib-d8

• 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].

• 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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C (Powder, protect from light, stored under nitrogen)

• Scientific Category:

  Isotope-Labeled Compounds

• Clinical Information:

  No Development Reported

• CAS Number:

  [1795134-78-9]