| Name | SU14813 maleate |
| Description | SU14813 maleate is an inhibitor of multi-targeted receptor tyrosine kinases (IC50s: 2, 50, 4, 15 nM for VEGFR1, VEGFR2, PDGFRβ, and KIT). |
| Cell Research | Passages 4 to 5 human umbilical vein endothelial cells are grown to subconfluency in EGM2 medium containing 10% FBS, endothelial cell growth supplement, and 10 μg/mL sodium heparin. The cells are seeded in 96-well plates at 10,000 per well in F12K medium and 10% FBS. The next day, cells are starved for 18 hours in F12K+1% FBS and then incubated with SU14813 in various concentrations. 45 minutes later, 20 ng/mL growth factor [VEGF or basic fibroblast growth factor (bFGF)] is introduced into the assay. Three days later, cell numbers are determined using the MTT assay. |
| Animal Research | SU14813 is evaluated for its efficacy and synergism in combination with the microtubule inhibitor docetaxel in docetaxel-resistant murine LLC model. SU14813 is administered p.o. twice daily (BID) at doses of 10, 40, 80, or 120 mg/kg beginning on day 5 after tumor implantation. Docetaxel 40 mg/kg (mouse maximum tolerated dose) is administered i.v. thrice-weekly also beginning on day 5 after tumor implantation. |
| In vitro | SU14813 inhibits cellular ligand-dependent phosphorylation of VEGFR-2 (transfected NIH 3T3 cells), PDGFR-β (transfected NIH 3T3 cells), KIT (Mo7e cells), and FLT3-internal tandem duplication (FLT3-ITD; MV4;11 cells) as well as FMS/CSF1R (transfected NIH 3T3 cells). SU14813 inhibits VEGFR-2, PDGFR-β, and KIT phosphorylation in porcine aorta endothelial cells overexpressing these targets, with cellular IC50 values of 5.2, 9.9, and 11.2 nM, respectively. SU14813 inhibits the growth of U-118MG (IC50: 50-100 nM). |
| In vivo | 'SU14813 inhibits VEGFR-2, PDGFR-β, and FLT3 phosphorylation in xenograft tumors in a dose- and time-dependent manner. The plasma concentration required for in vivo target inhibition is estimated to be 100 to 200 ng/mL. As monotherapy, SU14813 demonstrates broad and potent antitumor activity, causing regression, growth arrest, or substantially reduced growth of various established xenografts derived from human or rat tumor cell lines.' |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 3.3 mg/mL (5.91 mM), Sonication is recommended.
DMSO : 100 mg/mL (179.03 mM), Sonication is recommended.
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| Keywords | VEGFR2 | VEGFR1 | SU-14813 maleate | SU14813 maleate | SU 14813 Maleate | Kit | cKit |
| Inhibitors Related | Ribociclib | Gilteritinib | Sorafenib | Dasatinib | Pexidartinib | glycine | Nintedanib esylate | Regorafenib | Chloramphenicol | Thymoquinone | Lenvatinib | Pazopanib |
United States
