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
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
| 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 |
| SMILES string | Clc1ccc(cc1)NC(=O)c2c(cccc2)NCc3ccncc3 |
| 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 |
