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SU14813 maleate

SU14813 maleate
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SU14813 maleate

Catalog No. TQ0080Cas No. 849643-15-8
SU14813 maleate is an inhibitor of multi-targeted receptor tyrosine kinases (IC50s: 2, 50, 4, 15 nM for VEGFR1, VEGFR2, PDGFRβ, and KIT).
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Pack SizePriceAvailabilityQuantity
2 mg$535 days
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Product Introduction

Bioactivity
Description
SU14813 maleate is an inhibitor of multi-targeted receptor tyrosine kinases (IC50s: 2, 50, 4, 15 nM for VEGFR1, VEGFR2, PDGFRβ, and KIT).
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 fashion. The plasma concentration required for in vivo target inhibition is estimated to be 100 to 200 ng/mL. Used as monotherapy, SU14813 exhibits broad and potent antitumor activity resulting in regression, growth arrest, or substantially reduced growth of various established xenografts derived from human or rat tumor cell lines.
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.
Chemical Properties
Molecular Weight558.56
FormulaC27H31FN4O8
Cas No.849643-15-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 100 mg/mL (179.03 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7903 mL8.9516 mL17.9032 mL89.5159 mL
5 mM0.3581 mL1.7903 mL3.5806 mL17.9032 mL
10 mM0.1790 mL0.8952 mL1.7903 mL8.9516 mL
20 mM0.0895 mL0.4476 mL0.8952 mL4.4758 mL
50 mM0.0358 mL0.1790 mL0.3581 mL1.7903 mL
100 mM0.0179 mL0.0895 mL0.1790 mL0.8952 mL

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Preparation method for in vivo formula: Take 50 μLDMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μLTween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify.
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