PDGFR Tyrosine Kinase Inhibitor V-CAS 347155-76-4-Calbiochem

C₂₆H₂₃N₃O₄S · 3H₂O

527.59

MFCD12032139

A cell-permeable quinolinyl-thiourea compound that acts a potent, ATP-competitive, and reversible inhibitor of PDGFR (IC₅₀ = 4 and 7.6 nM in ligand-induced cellular PDGFR phosphorylation and in in vitro kinase activity, respectively). Inhibits c-kit receptor only at much higher concentrations (IC₅₀ = 434 and 234 nM in receptor phosphorylation and kinase activity, respectively). Shown to potently inhibit neointima formation in a rat carotid artery balloon injury model in vivo (30 mg/kg, p.o.).

Cell permeable: yes
Product competes with ATP.
Target IC₅₀: 4 and 7.6 nM in ligand-induced cellular PDGFR phosphorylation and in in vitro kinase activity, respectively
Primary Target
PDGFR
Reversible: yes

Toxicity: Toxic (F)

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

Getachew, R., et al. 2009. Eur. J. Pharmacol. In press.
Nishioka, C., et al. 2008. Blood111, 5086.
Furuta, T., et al. 2006. J. Med. Chem.49, 2186.
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CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
protect from light

off-white

DMSO: 25 mg/mL

ambient

2-8℃

1 mg in Plastic Bag(s)
Packaged under inert gas

11 - Combustible Solids

WGK 3