1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. SU1498

SU1498 (Synonyms: AG 1498; Tyrphostin SU 1498)

Cat. No.: HY-19326 Purity: 99.46%
Handling Instructions

SU1498 is a selective inhibitor of the VEGFR2; inhibits Flk-1 with an IC50 of value of 700 nM.

For research use only. We do not sell to patients.

SU1498 Chemical Structure

SU1498 Chemical Structure

CAS No. : 168835-82-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 82 In-stock
Estimated Time of Arrival: December 31
1 mg USD 60 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
25 mg USD 372 In-stock
Estimated Time of Arrival: December 31
50 mg USD 672 In-stock
Estimated Time of Arrival: December 31
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  • Protocol

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  • References

Description

SU1498 is a selective inhibitor of the VEGFR2; inhibits Flk-1 with an IC50 of value of 700 nM.

IC50 & Target[1]

Flk-1

700 nM (IC50)

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. The enhanced accumulation of phospho-ERKs is observed only in cells that have been stimulated with sphingosine 1-phosphate or protein growth factors; SU1498 by itself is ineffective[2]. SU1498 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[3]. SU1498 treatment significantly impacts U87 cell proliferation and apoptosis. SU1498 induces a marked increase in lipids and a decrease in glycerophosphocholine. Accordingly, accumulation of lipid droplets is seen in the cytoplasm of SU1498-treated U87 cells[4].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (384.10 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5607 mL 12.8034 mL 25.6069 mL
5 mM 0.5121 mL 2.5607 mL 5.1214 mL
10 mM 0.2561 mL 1.2803 mL 2.5607 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[2]

The ERK1 or ERK2 solution is pipetted into tubes (1 μL per tube) and mixed with 0-10 μL of 50 μM SU1498 (in kinase buffer without ATP). The blank tube receives buffer only. The volume is adjusted to 11 μL with the same buffer, and the mixtures are incubated for 10 min at 25°C. This is followed by the addition of 40 μL of the Elk1-ATP-buffer solution, and the incubations are continued for 30 min at 30°C. The reactions are stopped with 20 μL of 4× sample buffer mix and heating at 95°C for 10 min. Samples (15 μL) are fractionated by SDS-PAGE, and phosphorylated Elk1 is detected by immunoblotting with anti-phospho-Elk1 antibody[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[4]

For cell proliferation assay, 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[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

390.52

Formula

C₂₅H₃₀N₂O₂

CAS No.

168835-82-3

SMILES

O=C(NCCCC1=CC=CC=C1)/C(C#N)=C/C2=CC(C(C)C)=C(O)C(C(C)C)=C2

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
SU1498
Cat. No.:
HY-19326
Quantity:

SU1498

Cat. No.: HY-19326