JNJ-10198409 |
| カタログ番号GC14544 |
JNJ-10198409 は、比較的選択的で、経口活性があり、ATP と競合する PDGF-RTK (血小板由来増殖因子受容体チロシンキナーゼ) 阻害剤です (IC50=2 nM)。これは、デュアル メカニズム、抗血管新生、および腫瘍細胞増殖抑制剤です。 JNJ-10198409 は、PDGFR-β キナーゼ (IC50=4.2 nM) および PDGFR-α キナーゼ (IC50=45 nM) に対して良好な活性を示します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 627518-40-5
Sample solution is provided at 25 µL, 10mM.
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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.
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