627518-40-5
627518-40-5
Chemical Structure
JNJ-10198409
- CAS No.: 627518-40-5
- Formula:C18H16FN3O2
- Molecular Weight:325.34
IUPAC Name: N-(3-fluorophenyl)-6,7-dimethoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-amine
InChIKey: ZDNURMVOKAERHZ-UHFFFAOYSA-N
SMILES: COC1=CC2=C(C=C1OC)CC3=C2NN=C3NC4=CC=CC(F)=C4
Biological Activity: 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].
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JNJ-10198409 | 99.58% | 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). | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
