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Toceranib

Catalog No. T13178 CAS 356068-94-5

Synonyms: PHA 291639E, SU11654

Toceranib phosphate is an orally active inhibitor of tyrosine kinase (RTK) receptor, and it potently inhibits PDGFR, VEGFR, and Kit(with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively), has antitumor and antiangiogenic activity.

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Toceranib, CAS 356068-94-5

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Toceranib phosphate is an orally active inhibitor of tyrosine kinase (RTK) receptor, and it potently inhibits PDGFR, VEGFR, and Kit(with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively), has antitumor and antiangiogenic activity.
Targets&IC50	Flk-1:6 nM (ki), PDGFRβ:5 nM (ki)
In vivo	Administration of toceranib significantly decreased the number and percentage of Treg in the peripheral blood of dogs with cancer. Dogs receiving toceranib and CYC demonstrated a significant increase in serum concentrations of IFN-γ, which was inversely correlated with Treg numbers after 6 weeks of combination treatment[1].

Synonyms	PHA 291639E, SU11654
Molecular Weight	396.46
Formula	C22H25FN4O2
CAS No.	356068-94-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 2.4 mg/mL (6.05 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. 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. 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. 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.

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Toceranib 356068-94-5 Angiogenesis Tyrosine Kinase/Adaptors VEGFR c-Kit PDGFR PHA 291639E SCFR SU-11654 CD117 Vascular endothelial growth factor receptor SU 11654 inhibit Platelet-derived growth factor receptor Inhibitor SU11654 inhibitor

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