676483

VEGFR Tyrosine Kinase Inhibitor IV - CAS 475108-18-0 - Calbiochem

The VEGFR Tyrosine Kinase Inhibitor IV, also referenced under CAS 475108-18-0, controls the biological activity of VEGFR Tyrosine Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): VEGFR Tyrosine Kinase Inhibitor IV - CAS 475108-18-0 - Calbiochem, Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor IV, N-(2-Chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-Nʹ-(5-methyl-3-isoxazolyl)urea, PDGFR Tyrosine Kinase Inhibitor XII, VEGFR2 Kinase Inhibitor XXI, VEGFR1 Kinase Inhibitor, Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor IV, N-(2-Chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-Nʹ-(5-methyl-3-isoxazolyl)urea, PDGFR Tyrosine Kinase Inhibitor XII, VEGFR2 Kinase Inhibitor XXI, VEGFR1 Kinase Inhibitor V
• Empirical Formula (Hill Notation): C₂₂H₁₉ClN₄O₅ · xH₂O
• CAS Number: 475108-18-0
• Molecular Weight: 454.86 (anhydrous basis)
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: pink
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

General description

A cell-permeable quinoline-urea compound that potently inhibits the kinase activity of VEGFR (IC₅₀ = 30, 6.5, and 15 nM for VEGFR-1,-2, and -3, respectively), EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie-2 (IC₅₀ = 24, 40, 49, 78, and 78 nM, respectively). It exhibits little or no activity towards a panel of 15 other tyrosine kinases, including FGFR, IR, and IGFR, in cell-free kinase assays, while showing more than 7-fold higher potency in inhibiting ligand-induced phosphorylation of VEGFR-1/2/3 vs. c-Kit, PDGFR-β, Flt3, FGFR1, and c-Met in cell-based assays. Shown to be orally available and suppress tumor angiogenesis and growth in rats in vivo.

A cell-permeable quinoline-urea compound that potently inhibits the kinase activity of VEGFR (IC₅₀ = 30, 6.5, and 15 nM for VEGFR-1,-2,and -3, respectively), EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie-2 (IC₅₀ = 24, 40, 49, 78, and 78 nM, respectively). It exhibits little or no activity towards a panel of 15 other tyrosine kinases, including FGFR, IR, and IGFR, in cell-free kinase assays, while showing more than 7-fold higher potency in inhibiting ligand-induced phosphorylation of VEGFR-1/2/3 vs. c-Kit, PDGFR-β, Flt3, FGFR1, and c-Met in cell-based assays. Shown to be orally available and suppress tumor angiogenesis and growth in rats in vivo.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
VEGFR

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 30, 6.5, and 15 nM for VEGFR-1,-2, and -3, respectively; 24, 40, 49, 78, and 78 nM for EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie-2, respectively

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

Nakamura, K., et al. 2006. Cancer Res.66, 9134.

Legal Information

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

Safety Information

• Storage Class: 10-13 - German Storage Class 10 to 13