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JNJ-10198409

Catalog No.
C5737
inhibitor of platelet-derived growth factor (PDGF-BB) tyrosine kinase
Grouped product items
SizePriceStock Qty
5mg
$228.00
Ship with 5-10 days
10mg
$336.00
Ship with 5-10 days
50mg
$1,260.00
Ship with 5-10 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

JNJ-10198409 is a small molecule inhibitor of platelet-derived growth factor (PDGF-BB) tyrosine kinase [1].

Platelet-derived growth factor (PDGF) is a ubiquitous mitogen involved in regulating cell growth and division, embryonic development, cell proliferation, cell migration, and angiogenesis. Overexpression of PDGF has been associated with several diseases such as atherosclerosis, fibrotic disorders and malignancies. 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. Recombinant PDGF is used in medicine to help heal chronic ulcers and in orthopedic surgery and periodontistry to treat bone loss [2].

In human coronary artery smooth muscle cells, JNJ-10198409 inhibited the activity of platelet-derived growth factor (PDGF-BB) tyrosine kinase with an IC50 value of 4.2 nM when tested. JNJ-10198409 was a competitive antagonist of the ATP binding and hydrolysis at PDGF-BB receptor, resulting in a dose dependent inhibition of tumor growth and angiogenesis [1].

References:
[1] 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]. Journal of medicinal chemistry, 2005, 48(26): 8163-8173.
[2] Raines E W, Bowen-Pope D F, Ross R.  Platelet-derived growth factor[M]//Peptide growth factors and their receptors I. Springer Berlin Heidelberg, 1990: 173-262.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt 325.34
Cas No.627518-40-5
FormulaC18H16FN3O2
Solubility≤10mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
Chemical Name(Z)-N-(6,7-dimethoxy-1,2-dihydroindeno[1,2-c]pyrazol-3(4H)-ylidene)-3-fluoroaniline
SDFDownload SDF
Canonical SMILESCOC1=C(OC)C=C2C(CC3=C2NN/C3=N\C4=CC=CC(F)=C4)=C1
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

JNJ-10198409