Toceranib phosphate (C09-1074-260)

InformationToceranib phosphate (Palladia, SU11654), the phosphate salt of toceranib, is a selective inhibitor of thetyrosine kinaseactivity 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.TargetsPDGFR (Cell-free assay); Flk-1/DFR (Cell-free asssay) 5 nM(Ki); 6 nM(Ki)In vitroToceranib (SU11654) competes directly with ATP at the intracellular kinase domain of the RTK, thus preventing tyrosine phosphorylation and subsequent signal transduction. 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 vivoIn 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.Cell Research(from reference)Cell lines：BR, C2, and P815 cells Concentrations：0.01 to 1 μM Incubation Time：24, 48, and 72 hours. Specification: 0.98 Molecular Formula: C22H25FN4O2.H3O4P Molecular Weight: 494.45 PubChem CID: 16034840 Isomeric SMILES: CC1=C(NC(=C1C(=O)NCCN2CCCC2)C)/C=C/3/C4=C(C=CC(=C4)F)NC3=O.OP(=O)(O)O Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/T413259-SCI_3ed6c9ac6c230b87b9655684bae73bd8.pdf