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JNJ-10198409 Sale

(Synonyms: 3-氟-N-(6,7-二甲氧基-2,4-二氢茚并[1,2-C〕吡唑-3-基)苯基胺) 目录号 : GC14544

A potent PDGF tyrosine kinase inhibitor

JNJ-10198409 Chemical Structure

Cas No.:627518-40-5

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1mg
¥381.00
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5mg
¥1,634.00
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10mg
¥2,903.00
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50mg
¥12,610.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

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

Cas No. 627518-40-5 SDF
别名 3-氟-N-(6,7-二甲氧基-2,4-二氢茚并[1,2-C〕吡唑-3-基)苯基胺
化学名 (Z)-N-(6,7-dimethoxy-1,2-dihydroindeno[1,2-c]pyrazol-3(4H)-ylidene)-3-fluoroaniline
Canonical SMILES COC1=C(OC)C=C2C(CC3=C2NN/C3=N\C4=CC=CC(F)=C4)=C1
分子式 C18H16FN3O2 分子量 325.34
溶解度 ≤10mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide 储存条件 Store at -20°C
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1 mM 3.0737 mL 15.3685 mL 30.7371 mL
5 mM 0.6147 mL 3.0737 mL 6.1474 mL
10 mM 0.3074 mL 1.5369 mL 3.0737 mL
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