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

SU1498  (Synonyms: AG 1498; Tyrphostin SU 1498)

Cat. No.: HY-19326 Purity: 98.01%
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SU1498 (AG 1498) 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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
1 mg USD 45 In-stock
5 mg USD 90 In-stock
10 mg USD 150 In-stock
25 mg USD 310 In-stock
50 mg USD 500 In-stock
100 mg USD 800 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

SU1498 Related Antibodies

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

View All Isoforms
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

SU1498 (AG 1498) is a selective inhibitor of the VEGFR2; inhibits Flk-1 with an IC50 of value of 700 nM[1].

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].

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

SU1498 Related Antibodies
Molecular Weight

390.52

Formula

C25H30N2O2
CAS No.
Appearance

Solid

Color

White to off-white

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.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (256.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (6.40 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5607 mL 12.8034 mL 25.6069 mL 64.0172 mL
5 mM 0.5121 mL 2.5607 mL 5.1214 mL 12.8034 mL
10 mM 0.2561 mL 1.2803 mL 2.5607 mL 6.4017 mL
15 mM 0.1707 mL 0.8536 mL 1.7071 mL 4.2678 mL
20 mM 0.1280 mL 0.6402 mL 1.2803 mL 3.2009 mL
25 mM 0.1024 mL 0.5121 mL 1.0243 mL 2.5607 mL
30 mM 0.0854 mL 0.4268 mL 0.8536 mL 2.1339 mL
40 mM 0.0640 mL 0.3201 mL 0.6402 mL 1.6004 mL
50 mM 0.0512 mL 0.2561 mL 0.5121 mL 1.2803 mL
60 mM 0.0427 mL 0.2134 mL 0.4268 mL 1.0670 mL
80 mM 0.0320 mL 0.1600 mL 0.3201 mL 0.8002 mL
100 mM 0.0256 mL 0.1280 mL 0.2561 mL 0.6402 mL
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SU1498 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SU1498168835-82-3AG 1498 Tyrphostin SU 1498SU 1498SU-1498AG1498AG-1498Tyrphostin SU1498Tyrphostin SU 1498Tyrphostin SU-1498VEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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