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JNJ-10198409
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
JNJ-10198409图片
CAS NO: 627518-40-5
包装与价格：
包装 价格(元)
1mg 电议
5mg 电议
10mg 电议
50mg 电议

半岛bd体育手机客户端 介绍
JNJ-10198409 是一种相对选择性、口服活性和 ATP 竞争性的 PDGF-RTK（血小板衍生生长因子受体酪氨酸激酶）抑制剂 (IC50=2 nM)。它是一种双重机制、抗血管生成和肿瘤细胞抗增殖剂。 JNJ-10198409 对 PDGFR-β 激酶 (IC50=4.2 nM) 和 PDGFR-α 激酶 (IC50=45 nM) 具有良好的活性。
Cas No. 627518-40-5
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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 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.
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