For research use only. Not for therapeutic Use.
JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM)[1][2].
JNJ-10198409 has potent antiproliferative activity in six of eight human tumor cell lines (IC50<0.033 μM) and is a potent inhibitor of the c-Abl kinase (IC50=22 nM)[1][2].
| Catalog Number | I011729 |
| CAS Number | 627518-40-5 |
| Synonyms | N-(3-fluorophenyl)-6,7-dimethoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-amine |
| Molecular Formula | C18H16FN3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C18H16FN3O2/c1-23-15-7-10-6-14-17(13(10)9-16(15)24-2)21-22-18(14)20-12-5-3-4-11(19)8-12/h3-5,7-9H,6H2,1-2H3,(H2,20,21,22) |
| InChIKey | ZDNURMVOKAERHZ-UHFFFAOYSA-N |
| SMILES | COC1=C(C=C2C(=C1)CC3=C2NN=C3NC4=CC(=CC=C4)F)OC |
| Reference | [1]. D’Andrea MR, et al. Validation of in vivo pharmacodynamic activity of a novel PDGF receptor tyrosine kinase inhibitor using immunohistochemistry and quantitative image analysis. Mol Cancer Ther. 2005 Aug;4(8):1198-204. [2]. Ho CY, et al. (6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. J Med Chem. 2005 Dec 29;48(26):8163-73. |
