521237

PDGFR Tyrosine Kinase Inhibitor VII

The PDGFR Tyrosine Kinase Inhibitor VII, also referenced under CAS 251356-45-3, controls the biological activity of PDGFR Tyrosine Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): PDGFR Tyrosine Kinase Inhibitor VII, (Z)-3-(2,4-Dimethyl-5-(2-oxo-1,2-dihydro-indol-3-ylidenemethyl-6-phenyl)-1H-pyrrol-3-yl)-propionic acid, VEGFR Tyrosine Kinase Inhibitor XXXI, VEGFR2 Kinase Inhibitor XXIX
• Empirical Formula (Hill Notation): C₂₄H₂₂N₂O₃
• CAS Number: 251356-45-3
• Molecular Weight: 386.44
• UNSPSC Code: 12352200
• Assay: ≥97% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• Quality Segment: 100
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: dark orange
• solubility: DMSO: 25 mg/mL, ethanol: insoluble
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C24H22N2O3/c1-14-18(10-11-23(27)28)15(2)25-21(14)13-20-19-9-8-17(12-22(19)26-24(20)29)16-6-4-3-5-7-16/h3-9,12-13,25H,10-11H2,1-2H3,(H,26,29)(H,27,28)/b20-13-
• InChI key: APYYTEJNOZQZNA-MOSHPQCFSA-N

Description

General description

A cell-permeable indolinone compound that acts as a potent, ATP site-targeting PDGFR inhibitor (IC₅₀ = 10 nM against PDGFRβ), while affecting Flk-1/KDR/ VEGFR2, FGFR1, and EGFR only at much higher concentrations (IC₅₀ = 0.14, 2.29, and >100 µM, respectively). Reported to selectively inhibit PDGFβ- over EGF-stimulated proliferation in EGFR-expressing NIH 3T3 cultures (IC₅₀ = 0.11 and 21.9 µM, respectively) and exhibit much weaker potency against the proliferation of HUVEC cells upon FGF or VEGF stimulation (IC₅₀ = 10 µM).

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Sun, L., et al. 1999. J. Med. Chem.42, 5120.

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
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable