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Sigma-Aldrich

PDGFR Tyrosine Kinase Inhibitor IV

Synonym(s):

PDGFR Tyrosine Kinase Inhibitor IV, 3-Fluoro-N-(6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine, JNJ-10198409

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About This Item

Empirical Formula (Hill Notation):
C18H16FN3O2
CAS Number:
627518-40-5
Molecular Weight:
325.34
UNSPSC Code:
12352200
NACRES:
NA.77

Assay

≥98% (HPLC)

Quality Level

100

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 10 mg/mL
methanol: 5 mg/mL

shipped in

ambient

storage temp.

−20°C

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

General description

A cell-permeable indenopyrazole compound that displays potent antiproliferative properties in several human tumor cell lines (IC50<33 nM). Shown to act as an ATP-competitive and reversible inhibitor of PDGFR (IC50 = 4.2 nM and 45 nM for -β and -α, respectively) and c-Abl (IC50 = 22 nM). Exhibits less activity towards Lck, c-Src, and Fyn (IC50 = 100 nM, 185 nM and 378 nM, respectively) and exhibits little or no inhibition toward VEGFR, HER-2, Cdk′s-1,-2,-4 &-7, bFGFR-1 and EGFR (IC50 = 3.1 µM, >10 µM, >10 µM, 45.8 µM and >100 µM, respectively).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
PDGFR Tyrosine Kinase
Product competes with ATP.
Reversible: yes
Target IC50: 4.2 nM and 45 nM for -β and -α form of PDGFR, respectively

Packaging

Packaged under inert gas

Warning

Toxicity: Harmful (C)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Ho, C.Y., et al. 2005. J. Med. Chem.48, 8163.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

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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