676481

VEGFR Tyrosine Kinase Inhibitor II

The VEGFR Tyrosine Kinase Inhibitor II, also referenced under CAS 269390-69-4, 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 II, N-(4-Chlorophenyl)-2-[(pyridin-4-ylmethyl)amino]benzamide, VEGF Receptor Tyrosine Kinase Inhibitor II, VEGFR2 Kinase Inhibitor XVII, VEGFR1 Kinase Inhibitor III
• Empirical Formula (Hill Notation): C₁₉H₁₆ClN₃O
• CAS Number: 269390-69-4
• Molecular Weight: 337.80
• UNSPSC Code: 12352200
• NACRES: NA.54

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 5 mg/mL; methanol: soluble
• shipped in: wet ice
• storage temp.: −20°C
• InChI: 1S/C19H16ClN3O/c20-15-5-7-16(8-6-15)23-19(24)17-3-1-2-4-18(17)22-13-14-9-11-21-12-10-14/h1-12,22H,13H2,(H,23,24)
• InChI key: GGPZCOONYBPZEW-UHFFFAOYSA-N

Description

General description

A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the kinase activities of KDR, Flt-1 and c-Kit (IC₅₀ = 20 nM, 180 nM and 240 nM, respectively), and minimally inhibit c-Src and EGF-R activities (IC₅₀ = 7.0 µM and 7.3 µM). Also displays antiangiogenic and antitumor properties. Does not inhibit the activities of CDK-1, c-Met, IGF-1R or PKA (IC₅₀ >10 µM).

A pyridinyl-anthranilamide compound that displays both antiangiogenic and antitumor properties. A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the kinase activities of KDR, Flt-1 and c-Kit (IC₅₀ = 20 nM, 180 nM and 240 nM, respectively), and minimally inhibit c-Src and EGF-R activities (IC₅₀ = 7 µM and 7.3 µM). Further, inactive towards the inhibition of CDK-1, c-Met, IGF-1R and PKA (IC₅₀ >10 µM).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
Kinase activities of KDR, Flt-1 and c-Kit

Product competes with ATP.

Reversible: yes

Target IC₅₀: 20 nM, 180 nM and 240 nM against kinase activities of KDR, Flt-1 and c-Kit, 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 6 months at -20°C.

Other Notes

Furet, P., et al. 2003. Bioorg. Med. Chem. Lett.13, 2967.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable