Home Protein Tyrosine Kinase VEGFR inhibitor Toceranib phosphate

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Toceranib phosphate VEGFR inhibitor

Cat.No.S5272

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 VEGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 494.45

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 2 mg/mL (4.04 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 2 mg/mL

Ethanol : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 494.45 Formula

C22H25FN4O2.H3O4P

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 874819-74-6 -- Storage of Stock Solutions

Synonyms Palladia, SU11654 Smiles CC1=C(NC(=C1C(=O)NCCN2CCCC2)C)C=C3C4=C(C=CC(=C4)F)NC3=O.OP(=O)(O)O

Mechanism of Action

Targets/IC50/Ki
PDGFR
(Cell-free assay)
5 nM(Ki)
Flk-1/DFR
(Cell-free asssay)
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.
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.
References

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