627518-40-5

627518-40-5 structure

Name: JNJ-10198409
Chemical Name: N-(3-fluorophenyl)-6,7-dimethoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-amine
CAS Number: 627518-40-5
Molecular Formula: C₁₈H₁₆FN₃O₂
Molecular Weight: 325.337
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK PDGFR
Create Date: 2016-09-02 17:09:37
Modify Date: 2024-01-13 14:43:47
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].

Name	N-(3-fluorophenyl)-6,7-dimethoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-amine
Synonyms	Indeno[1,2-c]pyrazol-3-amine, N-(3-fluorophenyl)-2,4-dihydro-6,7-dimethoxy- (6,7-dimethoxy-2,4-dihydroindeno(1,2-c)pyrazol-3-yl)(3-fluorophenyl)amine N-(3-Fluorophenyl)-6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-amine PDGF Receptor Tyrosine Kinase Inhibitor IV 3-Fluoro-N-(6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine

Description	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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR
Target	PDGFRβ:4.2 nM (IC50) PDGFRα:45 nM (IC50)
In Vitro	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].
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. [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.

RIDADR	NONH for all modes of transport