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Chemical Structure| 168835-82-3 Chemical Structure| 168835-82-3

Structure of SU1498
CAS No.: 168835-82-3

Chemical Structure| 168835-82-3

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SU1498 is a selective inhibitor of the VEGFR2 with IC50 of 700 nM.

Synonyms: AG 1498; Tyrphostin SU 1498

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Product Details of SU1498

CAS No. :168835-82-3
Formula : C25H30N2O2
M.W : 390.52
SMILES Code : O=C(NCCCC1=CC=CC=C1)/C(C#N)=C/C2=CC(C(C)C)=C(O)C(C(C)C)=C2
Synonyms :
AG 1498; Tyrphostin SU 1498
MDL No. :MFCD03453026
InChI Key :JANPYFTYAGTSIN-FYJGNVAPSA-N
Pubchem ID :5941539

Safety of SU1498

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Related Pathways of SU1498

RTK

Isoform Comparison

Biological Activity

Description
SU1498 (AG 1498) is a selective VEGFR2 inhibitor, inhibiting Flk-1 with an IC50 value of 700 nM[1].

In Vitro:

Cell Line
Concentration Treated Time Description References
Astrocytes 20 μM 20 minutes SU1498 blocked VEGF-induced increase in PKCα phosphorylation PMC6594043
Hippocampal neurons 10 μM 2 to 24 hours To investigate the effects of VEGFR-2 inhibition on neuronal survival, results showed that SU1498 treatment led to decreased cell viability, oxidative stress, and mitochondrial dysfunction. PMC3756493
Mouse embryonic cortical neurons 1–100 μM 24 hours SU1498 inhibited VEGF's ability to stimulate BrdUrd labeling via VEGFR2/Flk-1 receptors PMC129374
Endothelial colony forming cells (ECFCs) 1 μM 24 hours Inhibited P2Y1 receptor agonist (10 μM 2MS-ATP)-induced angiogenesis, reducing stimulation from ~2.6-fold to 1.9-fold control; inhibited VEGF (262 pM)-induced angiogenesis, reducing stimulation from ~2.4-fold to 1.5-fold control PMC2694426
Human cardiac endothelial cells (HCECs) 1 μM 24 hours Inhibited P2Y1/2 receptor agonist (100 μM ATP or 10 μM 2MS-ATP)-induced angiogenesis, reducing stimulation to ~1.3-fold control levels PMC2694426
Endothelial cells 5–20 μM 3 days Inhibition of VEGF signaling, blocking the protective effects of NSPC conditioned medium on endothelial cells under conditions of serum starvation and OGD PMC3018350
Mouse brain endothelial cells (MBECs) 5 µM 5 hours SU1498, a specific VEGFR2 antagonist, abolished the angiogenesis enhanced by the supernatant from rhEPO-treated neural progenitor cells. PMC3971950

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice VEGFR-1 deficient mice Intraperitoneal injection 100 µl (100 mM in DMSO) Daily injections from P7 to P20 Inhibition of VEGFR-2 kinase activity reduced angiogenesis in VEGFR-1 deficient mice PMC3442373
Sprague-Dawley rats Chronic unpredictable stress model Intracerebroventricular injection 4 mM Administered on days 14, 16, 18, and 20 SU1498 completely blocked the antidepressant effects of fluoxetine in the sucrose preference test, novelty suppressed feeding test, and forced swim test PMC3694572
Mice Newborn Mice model Subcutaneous injection 30 mg/kg Single dose To study the inhibitory effect of SU1498 on alveolar development, results showed SU1498-treated mice had attenuated alveolar development with enlarged alveolar volume and sparse, dysmorphic capillaries. PMC2715334
C57BL/6J mice Wild-type and HDC-KO mice Intracerebroventricular injection 250 ng/2 mL Every 12 hours for a total of 3 injections SU1498 prevented the protective effect of hypoxic preconditioning in infarct volume and reversed the increased peripheral CBF in WT mice PMC3049494

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.56mL

0.51mL

0.26mL

12.80mL

2.56mL

1.28mL

25.61mL

5.12mL

2.56mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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