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

Properties

• 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

Description

General description

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 p60^c-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).

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 p60^c-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).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
VEGF-R2 (KDR/Flk-1)

Product competes with ATP.

Reversible: yes

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.

Other Notes

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 1