521233

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
• Empirical Formula (Hill Notation): C₁₈H₁₆FN₃O₂
• CAS Number: 627518-40-5
• Molecular Weight: 325.34
• MDL number: MFCD11045292
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Properties

• assay: ≥98% (HPLC)
• Quality Segment: 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
• SMILES string: Fc1cc(ccc1)Nc2[nH]nc3c2Cc4c3cc(c(c4)OC)OC
• 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

Description

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

Preparation Note

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

Disclaimer

Toxicity: Harmful (C)

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3