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J4649

JNJ-10198409

Name: JNJ-10198409
Brand: SIGMA

≥98% (HPLC), solid

Synonym(s):

3-Fluoro-N-(6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine, N-(3-fluorophenyl)-2,4-dihydro-6,7-dimethoxy-Indeno[1,2-c]pyrazol-3-amine, RWJ 540973

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About This Item

Empirical Formula (Hill Notation):

C₁₈H₁₆FN₃O₂

CAS Number:

627518-40-5

Molecular Weight:

325.34

UNSPSC Code:

51111800

PubChem Substance ID:

329815736

NACRES:

NA.77

Assay

≥98% (HPLC)

form

solid

color

off-white

solubility

DMSO: >10 mg/mL
H₂O: <2 mg/mL

originator

Johnson & Johnson

storage temp.

−20°C

SMILES string

COc1cc2Cc3c(Nc4cccc(F)c4)n[nH]c3-c2cc1OC

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)

InChI key

ZDNURMVOKAERHZ-UHFFFAOYSA-N

Biochem/physiol Actions

JNJ-10198409 is a potent ATP-competitive inhibitor of Platelet-Derived Growth Factor receptor tyrosine kinase (PDGF-RTK) with both antiangiogenicand a directtumor cell antiproliferative activity. It is selective for PDGF-β kinase with IC₅₀ values of 4.2 nM for PDGF-β and 45 nM for PDGF-α kinase.

Features and Benefits

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound is featured on the PAF Receptor and PDGFR pages of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Johnson & Johnson. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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(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.

Chih Y Ho et al.

Journal of medicinal chemistry, 48(26), 8163-8173 (2005-12-22)

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 tyrosine kinase of Platelet-Derived Growth Factor-BB (PDGF-BB), and to improve the broad tumor cell antiproliferative activity of these compounds. This

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

Michael R D'Andrea et al.

Molecular cancer therapeutics, 4(8), 1198-1204 (2005-08-12)

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 objective of the present study was to determine if we

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