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521237 Sigma-Aldrich

PDGFR Tyrosine Kinase Inhibitor VII - CAS 251356-45-3 - Calbiochem

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: (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, PDGFR Tyrosine Kinase Inhibitor VII - CAS 251356-45-3 - Calbiochem

  • CAS Number 251356-45-3

  • Empirical Formula (Hill Notation) C24H22N2O3

  • Molecular Weight 386.44

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Properties

Related Categories Biochemicals and Reagents, Enzyme Inhibitors, Enzyme Inhibitors by Enzyme, Enzymes, Inhibitors, and Substrates, P to Q,
Quality Level   100
assay   ≥97% (HPLC)
form   solid
mfr. no.   Calbiochem®
storage condition   OK to freeze
  protect from light
storage conditions   +2C to +8C
color   dark orange
solubility   DMSO: 25 mg/mL
  ethanol: insoluble
shipped in   ambient

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

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

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

Safety & Documentation

Safety Information

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