Catalog No.S5272 Synonyms: Palladia, SU11654
Molecular Weight(MW): 494.45
Toceranib phosphate, 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.
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|Description||Toceranib phosphate, 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 (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.|
|In vitro||DMSO||2 mg/mL (4.04 mM)|
|Water||2 mg/mL (4.04 mM)|
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