Toceranib

Toceranib phosphate (SU11654 phosphate) 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 phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors[1][2].

Product Specifications

CAS Number

[356068-94-5]

Product Name Alternative

SU11654; PHA 291639E

UNSPSC

12352005

Hazard Statement

H315, H319

Target

C-Kit; PDGFR; VEGFR

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Toceranib.html

Purity

97.41

Solubility

DMSO : 2.5 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL

Smiles

O=C(NCCN1CCCC1)C2=C(NC(/C=C3C(NC4=C\3C=C(C=C4)F)=O)=C2C)C

Molecular Formula

C22H25FN4O2

Molecular Weight

396.46

Precautions

H315, H319

References & Citations

[1]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.|[2]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.|[3]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.