Toceranib phosphate

Catalog No.S5272 Batch:S527201

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.

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.

References

RETURN POLICY
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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.

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