Catalog No. C5737

JNJ-10198409

血小板衍生生长因子（PDGF-BB）酪氨酸激酶抑制剂

规格	价格	货期
5mg	请咨询	10-15工作日发货
10mg	请咨询	10-15工作日发货
50mg	请咨询	10-15工作日发货

CAS号：627518-40-5纯度：98.00%

仅用于科研，不用于诊疗。未经明确授权不得转售。

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特色产品

Annexin V-FITC/PI Apoptosis Kit

用于双染检测细胞凋亡和坏死

- 在10-20分钟内完成染色
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞

Phos binding reagent (Phosbind) acrylamide

分离和检测磷酸化/非磷酸化蛋白

- 新型的磷酸盐结合标签和功能分子
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白

Cell Counting Kit-8 (CCK-8)

用于细胞增殖和细胞毒性试验

- 比MTT，MTS或WST-1更敏感
- 对细胞无毒性
- 步骤更简单，无需有机溶剂

Cy5 TSA Fluorescence System Kit

Cy5荧光标记的酪胺信号放大系统

- 检测ICC/IHC/ISH中的低丰度靶点
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率

EZ Cap™ Cy5 Firefly Luciferase mRNA (5-moUTP)

用于观察mRNA运送，定位，翻译

- 具有Cap1结构的荧光素酶mRNA
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰

HotStart™ 2X Green qPCR Master Mix

用于荧光定量目标DNA或cDNA

- 通过热启动机制优化扩增特异性
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单

HyperScribe™ T7 High Yield Cy5 RNA Labeling Kit Plus

高效的Cy5修饰RNA转录试剂盒

- 适合原位/Northernblot杂交实验
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量

产品描述产品性质产品应用质量控制操作说明产品引用文献摩尔浓度计算器

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.

产品性质

物理外观	A crystalline solid
CAS号	627518-40-5
分子式	C₁₈H₁₆FN₃O₂
分子量	325.34
化学名称	(Z)-N-(6,7-dimethoxy-1,2-dihydroindeno[1,2-c]pyrazol-3(4H)-ylidene)-3-fluoroaniline
溶解度	≤10mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
SMILES	COc(cc(CC1=C2NN/C\1=N\c1cccc(F)c1)c2c1)c1OC
存储条件	-20°C
运输条件	蓝冰

产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)

IC50和靶点

生物活性描述

JNJ-10198409 是一种具有相对选择性、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）。它是一种双机制、抗血管生成和抗肿瘤细胞增殖的药物。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。