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SU1498

Cat. No. M8916
SU1498 Structure
Synonym:

AG-1498

Size Price Availability
10mg USD 200 4-7 Days
50mg USD 750 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

SU-1498 is a selective inhibitor of the VEGFR2, which inhibits Flk-1 with an IC50 value of 700 nM.

In vitro: SU1498 stimulates accumulation of phosphorylated ERKs in human umbilical vein endothelial cells and in human aortic endothelial cells in a manner that is dependent on the functioning of the upstream components of the MAPK pathway, B-Raf and MEK kinases. SU 1498 blocks signal transduction from VEGFR2 in MS1 VEGF cells. In the presence of SU1498, levels of Ets-1 are decreased, suggesting that VEGF-VEGFR-2 interactions contributed to baseline levels of Ets-1 expression, and interruption of this autocrine interaction with SU1498 led to decreased expression of Ets-1. SU1498 treatment significantly impacts U87 cell proliferation and apoptosis. SU-1498 induces a marked increase in lipids and a decrease in glycerophosphocholine.

Protocol
Cell Experiment
Cell lines U87 cells
Preparation method For cell proliferation assay, SU1498 is prepared as a stock solution of 30 mM in DMSO, then diluted with culture medium to working concentrations before use. U87 cells are seeded in 24-well plates (30,000 cells/well) and allowed to attach overnight. Cells are then treated for 24 or 72 h with different concentrations of Bevacizumab (from 10 ng/mL to 250 µg/mL) or SU1498 (from 1 µM to 30 µM) in triplicate wells. The cell viability is then assessed with the MTT assay.
Concentrations From 1 µM to 30 µM
Incubation time 24 or 72 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 390.52
Formula C25H30N2O2
CAS Number 168835-82-3
Purity >98%
Solubility DMSO: 100 mg/mL
Storage at -20°C
References

Metabolic impact of anti-angiogenic agents on U87 glioma cells.
Mesti T, et al. PLoS One. 2014 Jun 12;9(6):e99198. PMID: 24922514.

SU1498, an inhibitor of vascular endothelial growth factor receptor 2, causes accumulation of phosphorylated ERK kinases and inhibits their activity in vivo and in vitro.
Boguslawski G, et al. J Biol Chem. 2004 Feb 13;279(7):5716-24. PMID: 14625306.

Overexpression of VEGF 121 in immortalized endothelial cells causes conversion to slowly growing angiosarcoma and high level expression of the VEGF receptors VEGFR-1 and VEGFR-2 in vivo.
Arbiser JL, et al. Am J Pathol. 2000 Apr;156(4):1469-76. PMID: 10751370.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SU1498, AG-1498 supplier, VEGFR/PDGFR, inhibitors

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