General description
A cell-permeable pyrrole-indolinone compound that acts as a potent, reversible, and ATP-competitive tyrosine kinase receptor and angiogenic inhibitor that exhibits greater selectivity for PDGFRβ (IC50 = 3 nM), VEGFR2 (IC50 = 27 nM), FGFR1 (IC50 = 170 nM), and Kit family members (IC50 = ~ 10-500 nM) over EGFR (IC50 >20 µM). Reported to display anti-proliferative and pro-apoptotic properties in tumor cells.
A cell-permeable, potent, reversible, and ATP-competitive inhibitor of tyrosine kinase activity of PDGFRβ (IC50 = 3 nM), VEGFR2 (IC50 = 27 nM), FGFR1 (IC50 = 170 nM), and Kit family members (IC50 ~10-500 nM). Does not effect the activity of EGFR (IC50 >20 µM). Reported to display anti-proliferative, antiangiogenic and pro-apoptotic properties in tumor cells.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PDGFRB
Product competes with ATP.
Reversible: yes
Target IC50: 3 nM, 27 nM, 170 nM against PDGFRβ, VEGFR2, and FGFR1, 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
Heryanto, B., et al. 2003. Reproduction125, 334.
Sun, L., et al. 2003. J. Med. Chem.46, 1116.
Liao, A.T., et al. 2002. Blood100, 585.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥95% (HPLC) |
| form | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | orange |
| solubility | DMSO: 4 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | Clc1cc2c(cc1)NC(=O)\C\2=C/c3[nH]c(c(c3C)C(=O)NCCN(CC)CC)C |
| InChI | 1S/C22H27ClN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12- |
| InChI key | XPLJEFSRINKZLC-ATVHPVEESA-N |
