Home Protein Tyrosine Kinase VEGFR inhibitor - PDGFR inhibitor Toceranib phosphate For research use only.

Toceranib phosphate

Synonyms: Palladia, SU11654

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.

Toceranib phosphate Chemical Structure

Toceranib phosphate Chemical Structure

CAS No. 874819-74-6

Purity & Quality Control

Batch: S527201 DMSO]2 mg/mL]false]Water]2 mg/mL]false]Ethanol]Insoluble]false Purity: 99.87%
99.87

Toceranib phosphate Related Products

Signaling Pathway

VEGFR Signaling Pathways

VEGFR Signaling Pathway

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
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].
Cell Research 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.
In Vivo
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].

Chemical Information & Solubility

Molecular Weight 494.45 Formula

C22H25FN4O2.H3O4P
CAS No. 874819-74-6 SDF --
Smiles CC1=C(NC(=C1C(=O)NCCN2CCCC2)C)C=C3C4=C(C=CC(=C4)F)NC3=O.OP(=O)(O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 2 mg/mL ( (4.04 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 2 mg/mL

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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