JNJ-10198409

JNJ-10198409用途

JNJ-10198409 是一种相对选择性的,具有口服活性的,ATP 竞争性的血小板衍生生长因子受体酪氨酸激酶 (PDGF-RTK) 抑制剂 (IC50=2 nM)。它是一种双重机制的抗血管生成和肿瘤细胞的抗增殖剂。JNJ-10198409 对 PDGFR-β 激酶 (IC50=4.2 nM) 和 PDGFR-α 激酶 (IC50=45 nM) 有较好的抑制作用。

JNJ-10198409名称

[ CAS 号 ]:
627518-40-5

[ 英文名 ]:
JNJ-10198409

[英文别名 ]:

PDGF Receptor Tyrosine Kinase Inhibitor IV

JNJ-10198409生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 蛋白酪氨酸激酶 >> PDGFR

[ 靶点 ]

PDGFRβ:4.2 nM (IC50)

PDGFRα:45 nM (IC50)

[体外研究]

JNJ-10198409在8种人肿瘤细胞系中的6种中具有有效的抗增殖活性(IC50<0.033μM),并且是c-Abl激酶的有效抑制剂(IC50=22nM)[1][2]。

[参考文献]

[1]. D'Andrea MR, et al. Validation of in vivo pharmacodynamic activity of a novel PDGF receptor tyrosine kinase inhibitor using immunohistochemistry and quantitative image analysis. Mol Cancer Ther. 2005 Aug;4(8):1198-204.

[2]. Ho CY, 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 Med Chem. 2005 Dec 29;48(26):8163-73.

JNJ-10198409物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
528.8±50.0 °C at 760 mmHg

[ 分子式 ]:
C₁₈H₁₆FN₃O₂

[ 分子量 ]:
325.337

[ 闪点 ]:
273.6±30.1 °C

[ 精确质量 ]:
325.122650

[ PSA ]:
62.40000

[ LogP ]:
3.91

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.671

JNJ-10198409MSDS

详细MSDS(安全技术说明书)

JNJ-10198409安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

JNJ-10198409文献

(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. Med. Chem. 48 , 8163-8173, (2005)

A series of (6,7-dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines has been optimized to preserve both potent kinase inhibition activity against the angiogenesis target, the receptor tyrosin...

Validation of in vivo pharmacodynamic activity of a novel PDGF receptor tyrosine kinase inhibitor using immunohistochemistry and quantitative image analysis.

Mol. Cancer Ther. 4 , 1198-1204, (2005)

With the advent of agents directed against specific molecular targets in drug discovery, it has become imperative to show a compound's cellular impact on the intended biomolecule in vivo. The objectiv...

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JNJ-10198409

JNJ-10198409用途

JNJ-10198409名称

JNJ-10198409生物活性

JNJ-10198409物理化学性质

JNJ-10198409MSDS

详细MSDS(安全技术说明书)

JNJ-10198409安全信息

JNJ-10198409文献

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相关化合物

JNJ-​10198409

JNJ-​10198409用途

JNJ-​10198409名称

JNJ-​10198409生物活性

JNJ-​10198409物理化学性质

JNJ-​10198409MSDS

详细MSDS(安全技术说明书)

JNJ-​10198409安全信息

JNJ-​10198409文献

推荐生产厂家/供应商：

相关化合物

JNJ-10198409

JNJ-10198409用途

JNJ-10198409名称

JNJ-10198409生物活性

JNJ-10198409物理化学性质

JNJ-10198409MSDS

JNJ-10198409安全信息

JNJ-10198409文献