Toceranib (phosphate)

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

[874819-74-6]

Product Name Alternative

SU11654 (phosphate) ; PHA 291639E (phosphate)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

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-phosphate.html

Purity

98.54

Solubility

DMSO : 2.46 mg/mL (ultrasonic; warming)

Smiles

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

Molecular Formula

C22H28FN4O6P

Molecular Weight

494.45

Precautions

H302, H315, H319, H335

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.|[4]London C, Mathie T, Stingle N, et al. Preliminary evidence for biologic activity of toceranib phosphate (Palladia (®) ) in solid tumours. Vet Comp Oncol. 2012;10 (3) :194-205.