JNJ-​10198409

Modify Date: 2024-01-13 14:43:47

JNJ-​10198409 Structure
JNJ-​10198409 structure
Common Name JNJ-​10198409
CAS Number 627518-40-5 Molecular Weight 325.337
Density 1.4±0.1 g/cm3 Boiling Point 528.8±50.0 °C at 760 mmHg
Molecular Formula C18H16FN3O2 Melting Point N/A
MSDS USA Flash Point 273.6±30.1 °C

 Use of JNJ-​10198409


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].

 Names

Name N-(3-fluorophenyl)-6,7-dimethoxy-1,4-dihydroindeno[1,2-c]pyrazol-3-amine
Synonym More Synonyms

 JNJ-​10198409 Biological Activity

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
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.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 528.8±50.0 °C at 760 mmHg
Molecular Formula C18H16FN3O2
Molecular Weight 325.337
Flash Point 273.6±30.1 °C
Exact Mass 325.122650
PSA 62.40000
LogP 3.91
Vapour Pressure 0.0±1.4 mmHg at 25°C
Index of Refraction 1.671

 Safety Information

RIDADR NONH for all modes of transport

 Articles2

More Articles
(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. 48 , 8163-8173, (2005)

A series of (6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines has been optimized to preserve both potent kinase inhibition activity against the angiogenesis target, the receptor tyrosin...

Validation of in vivo pharmacodynamic activity of a novel PDGF receptor tyrosine kinase inhibitor using immunohistochemistry and quantitative image analysis.

Mol. Cancer Ther. 4 , 1198-1204, (2005)

With the advent of agents directed against specific molecular targets in drug discovery, it has become imperative to show a compound's cellular impact on the intended biomolecule in vivo. The objectiv...

 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
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