Toceranib phosphate

Catalog No.S5272 Batch:S527201

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Technical Data

Formula

C22H25FN4O2.H3O4P
Molecular Weight 494.45 CAS No. 874819-74-6
Solubility (25°C)* In vitro DMSO 2 mg/mL (4.04 mM)
Water 2 mg/mL (4.04 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Toceranib phosphate (Palladia, SU11654), the phosphate salt of toceranib, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively.
Targets
PDGFR [1]
(Cell-free assay)		 Flk-1/DFR [1]
(Cell-free asssay)
5 nM(Ki) 6 nM(Ki)
In vitro Toceranib (SU11654) competes directly with ATP at the intracellular kinase domain of the RTK, thus preventing tyrosine phosphorylation and subsequent signal transduction. In vitro, SU11654 exerts a potent antiproliferative effect on endothelial cells. Additionally, SU11654 treatment can induce cell cycle arrest and subsequent apoptosis in tumor cell lines expressing activating mutations in split kinase RTKs[1].
In vivo In mouse xenograft models, oral administration of SU11654 and related compounds affects the growth of multiple tumor cell lines originating from a variety of tissues, leading to either tumor regression or tumor growth inhibition[1].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    BR, C2, and P815 cells

  • Concentrations

    0.01 to 1 μM

  • Incubation Time

    24, 48, and 72 hours

  • Method

    The BR, C2, and P815 cells were counted and resuspended in 24-well plates at a concentration of 0.5 × 106 cells/well (BR and C2) or 0.25 × 106 cells/well (P815) in complete medium. Cells were left untreated, or SU11652, SU11654, or SU11655 was added to a final concentration of 0.01 to 1 μM. Cells were collected after 24, 48, and 72 hours of culture and were counted to determine the number of cells surviving.

Selleck's Toceranib phosphate has been cited by 1 publication

Establishment and characterization of six canine hepatocellular carcinoma cell lines [ Front Vet Sci, 2024, 11:1392728] PubMed: 38840628

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.