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Merck

676485

VEGFR2 Kinase Inhibitor II - CAS 288144-20-7 - Calbiochem

The VEGFR2 Kinase Inhibitor II, also referenced under CAS 288144-20-7, controls the biological activity of VEGFR2 Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

VEGFR2 Kinase Inhibitor II - CAS 288144-20-7 - Calbiochem, ( Z)-5-Bromo-3-(4,5,6,7-tetrahydro-1 H-indol-2-ylmethylene)-1,3-dihydroindol-2-one, Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor II, VEGFR Tyrosine Kinase Inhibitor XIII, (Z)-5-Bromo-3-(4,5,6,7-tetrahydro-1H-indol-2-ylmethylene)-1,3-dihydroindol-2-one, Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor II, VEGFR Tyrosine Kinase Inhibitor XIII

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About This Item

Empirical Formula (Hill Notation):
C17H15BrN2O
CAS Number:
288144-20-7
Molecular Weight:
343.22
UNSPSC Code:
12352200

Key Documents

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assay

≥95% (HPLC)

form

solid

potency

70 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

brown

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

−20°C

Biochem/physiol Actions

Cell permeable: yes
Primary Target
VEGF-R2 (KDR/Flk-1)
Product competes with ATP.
Reversible: yes

Disclaimer

Toxicity: Standard Handling (A)

General description

A membrane permeant and reversible indolin-2-one class of receptor tyrosine kinase (RTK) inhibitor [IC50 = 70 nM for VEGF-R2 (KDR/Flk-1), 920 nM for PDGF-Rβ, 4.92 µM for p60c-src, and 13.3 µM for FGF-R1]. The inhibition is suggested to be competitive with respect to ATP. Does not inhibit EGF-R kinase activity (IC50 >100 µM).
A cell-permeable and reversible indolin-2-one class of receptor tyrosine kinase (RTK) inhibitor [IC50 = 70 nM for VEGF-R2 (KDR/Flk-1), 920 nM for PDGF-Rβ, 4.92 µM for p60c-src, and 13.3 µM for FGF-R1]. The inhibition is suggested to be competitive with respective to ATP. Also inhibits VEGF-induced (IC50 = 110 nM) and PDGF-induced (IC50 = 2.01 µM) cell proliferation in umbilical vein endothelial cells (HUVEC). Does not exhibit any inhibitory effect on EGF-R kinase activity (IC50 >100 µM).

Other Notes

Sun, L., et al. 2000. J. Med. Chem.43, 2655.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 1

Certificates of Analysis (COA)

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Oisun Jung et al.
Journal of cell science, 132(20) (2019-09-29)
When targeted by the tumor-promoting enzyme heparanase, cleaved and shed syndecan-1 (Sdc1) then couples VEGFR2 (also known as KDR) to VLA-4, activating VEGFR2 and the directed migration of myeloma cells. But how VEGFR2 activates VLA-4-mediated motility has remained unknown. We now

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