A potent PDGF tyrosine kinase inhibitor
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JNJ-10198409

Item No. 10008131

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(3-fluorophenyl)-1,4-dihydro-6,7-dimethoxy-indeno[1,2-c]pyrazol-3-amine
CAS Number
627518-40-5
Molecular Formula
C18H16FN3O2
Formula Weight
325.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 10 mg/ml
λmax
267, 302 nm
SMILES
COc1cc2c(Cc3c(n[nH]c23)Nc2cccc(F)c2)cc1OC
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $31

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    5 mg

    $129

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    10 mg

    $228

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    50 mg

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    Product Description

    Inhibition of the tyrosine kinase activity of growth factor receptors such as the platelet-derived growth factor (PDGF-BB) receptor can have potent antiangiogenic and antiproliferative activity.1 JNJ-10198409 is a small molecule inhibitor of platelet-derived growth factor (PDGF-BB) tyrosine kinase with an IC50 value of 4.2 nM when tested in human coronary artery smooth muscle cells.2 JNJ-10198409 is a competitive antagonist of the ATP binding and hydrolysis at this receptor, resulting in a dose dependent inhibition of tumor growth and angiogenesis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Battegay, E.J., Rupp, J., Iruela-Arispe, L., et al. PDGF-BB modulates endothelial proliferation and angiogenesis in vitro via PDGF β-receptors. J. Cell Biol. 125(4), 917-928 (1994).

    2. Ho, C.Y., Ludovici, D.W., Maharoof, U.S.M., 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. 48(26), 8163-8173 (2005).