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PD184161

CAS号

212631-67-9

分子式

C17H13BrClF2IN2O2

主要靶点

MEK

仅限科研使用

Cat No : CM05067

Print datasheet

Synonyms

depressive|HCC|Apoptosis|behavioral|cancer|cell|stroke|inhibit|Inhibitor|MAPKK|MAP2K|MEK1/2|MEK|Mitogen-activated protein kinase kinase|neurons|PD184161|PD-184161|PD 184161

验证数据展示

  • CAS No.: 212631-67-9

    PD184161
    CAS#: 212631-67-9

产品信息

CAS号 212631-67-9
分子式 C17H13BrClF2IN2O2
主要靶点 MEK
主要通路 MAPK 信号通路
分子量 557.56
纯度 99.09%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 depressive|HCC|Apoptosis|behavioral|cancer|cell|stroke|inhibit|Inhibitor|MAPKK|MAP2K|MEK1/2|MEK|Mitogen-activated protein kinase kinase|neurons|PD184161|PD-184161|PD 184161

靶点活性

MEK1/2:10-100 nM

体内活性

在体内，肿瘤异种移植物P-ERK水平在口服PD184161后3至12小时内显著减少（P < .05）。相反，经过长期（24天）每日给药的PD184161处理后，肿瘤异种移植物P-ERK水平对这种信号效应变得不敏感。PD184161显著抑制了肿瘤的植入和初期生长（P < .0001）；然而，对已建立的肿瘤没有显著影响。总之，PD184161在体内对抗HCC显示出与抑制MEK活性相关的抗肿瘤效应[1]。

体外活性

PD184161 在时间和浓度依赖的方式中，较之 PD098059 或 U0126 更有效地抑制了 MEK 活性 (IC50 = 10-100 nM)。在大于或等于 1.0 microM 浓度下，PD184161 同样以时间和浓度依赖的方式抑制了细胞增殖并诱导了凋亡[1]。

溶解度

DMSO:55 mg/mL (98.64 mM)

参考文献

1.Klein, P. J.,Schmidt, C.M.,Wiesenauer, C.A., et al. The effects of a novel MEK inhibitor PD184161 on MEK-ERK signaling and growth in human liver cancer. Neoplasia 8(1), 1-8 (2006).

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