General description
A cell-permeable, reversible, ATP-competitive, and selective inhibitor of platelet-derived growth factor (PDGF) receptor kinase (IC50 = 500 nM) and PDGF-dependent DNA synthesis (IC50 = 2.5 µM) in Swiss/3T3 cells. Has no effect on EGF receptor autophosphorylation and shows only a weak effect on EGF- or insulin-stimulated DNA synthesis. A potent blocker of smooth muscle cell proliferation.
Selectively inhibits platelet-derived growth factor (PDGF) receptor kinase (IC50 = 500 nM) and the PDGF-dependent DNA synthesis (IC50 = 2.5 µM) in Swiss 3T3 cells. Has no effect on epidermal growth factor (EGF) receptor autophosphorylation and shows only a weak effect on EGF- or insulin-stimulated DNA synthesis.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PDGFR kinase
Product competes with ATP.
Reversible: yes
Target IC50: 500 nM against PDGFR kinase
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Other Notes
Banai, S., et al. 1998. Circulation 97, 1960.
Levitzki, A., and Gazit, A. 1995. Science267, 1782.
Kovalenko, M., et al. 1994. Cancer Res.54, 6106.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥95% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | white |
| solubility | DMSO: 10 mg/mL,dichloromethane: soluble |
| shipped in | ambient |
| storage temp. | −20°C |
| SMILES string | n1c2c(ncc1c3ccccc3)cc(c(c2)C)C |
| InChI | 1S/C16H14N2/c1-11-8-14-15(9-12(11)2)18-16(10-17-14)13-6-4-3-5-7-13/h3-10H,1-2H3 |
| InChI key | FQNCLVJEQCJWSU-UHFFFAOYSA-N |
