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CI-1040 {[allProObj[0].p_purity_real_show]}

货号：A832312 同义名： PD 184352

CI-1040（PD 184352）是一种口服活性、高度特异性的小分子MEK抑制剂，对MEK1的IC50为17 nM。

CI-1040 化学结构 CAS号：212631-79-3
CI-1040 化学结构
CAS号：212631-79-3
CI-1040 3D分子结构
CAS号：212631-79-3
CI-1040 化学结构 CAS号：212631-79-3
CI-1040 3D分子结构 CAS号：212631-79-3
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CI-1040 纯度/质量文件 产品仅供科研

货号：A832312 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 MEK ↓ MEK1 ↓ MEK1/2 ↓ MEK2 ↓ MEK5 ↓ 其他靶点 纯度
Honokiol ✔ 98%
Mirdametinib ++++

MEK, IC50: 0.33 nM

 		99%+
Binimetinib +++

MEK, IC50: 12 nM

 		99%+
BI-847325 ++

MEK1, IC50: 25 nM

 		+++

MEK2, IC50: 4 nM

 		99%+
U0126-EtOH +

MEK1, IC50: 0.07 μM

 		++

MEK2, IC50: 0.06 μM

 		98%
GDC-0623 ++++

MEK1, IC50: 0.13 nM

 		99%+
TAK-733 ++++

MEK1, IC50: 3.2 nM

 		99%+
Trametinib ++++

MEK1, IC50: 0.92 nM

 		++++

MEK2, IC50: 1.8 nM

 		99%+
Selumetinib +++

MEK1, IC50: 14 nM

MEK1, Kd: 99 nM

 		+

MEK2, Kd: 530 nM

 		99%+
CI-1040 ++

MEK1, IC50: 17 nM

 		++

MEK2, IC50: 17 nM

 		99%+
Myricetin ✔ 98%
Refametinib ++

MEK1, IC50: 19 nM

 		++

MEK2, IC50: 47 nM

 		99%+
Cobimetinib +++

MEK1, IC50: 4.2 nM

 		99%+
PD98059 +

MEK1, IC50: 2 μM

 		99%+
SL327 +

MEK1, IC50: 0.18 μM

 		+

MEK2, IC50: 0.22 μM

 		AP-1 98+%
PD318088 ✔ 98%
AZD8330 +++

MEK1/2, IC50: 7 nM

 		99%+
Pimasertib 98%
(E/Z)-BIX02189 ++++

MEK5, IC50: 1.5 nM

 		99%+
(E/Z)-BIX02188 +++

MEK5, IC50: 4.3 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

CI-1040 生物活性

靶点

  • MEK2

    MEK2, IC50:17 nM

  • MEK1

    MEK1, IC50:17 nM
描述 CI-1040 effectively inhibits MEK1 with an IC50 of 17 nM, displaying minimal activity against other related kinases, with IC50 values more than 2.5 orders of magnitude higher. This specificity allows CI-1040 to completely inhibit mitogen-stimulated phosphorylation of ERK in whole cells. Specifically, at a concentration of 1 μM, CI-1040 reduces phosphorylation of ERK1 and ERK2 by 99% and 92%, respectively, in MDA-MB-231 breast cancer cells[1]. CI-1040 also induces apoptosis and curtails proliferation in U-937 cells in a dose- and time-dependent manner, significantly elevating PUMA mRNA and protein levels, which are markers of apoptotic processes[2].
体内研究

When administered systemically, the MEK inhibitor CI-1040 markedly decreases adenoma formation by a third and effectively restores lung structure in mice. It also reduces the proliferation rate of lung cells without notably affecting the differentiation of pneumocytes[3].
体外研究

CI-1040 effectively inhibits MEK1 with an IC50 of 17 nM, displaying minimal activity against other related kinases, with IC50 values more than 2.5 orders of magnitude higher. This specificity allows CI-1040 to completely inhibit mitogen-stimulated phosphorylation of ERK in whole cells. Specifically, at a concentration of 1 μM, CI-1040 reduces phosphorylation of ERK1 and ERK2 by 99% and 92%, respectively, in MDA-MB-231 breast cancer cells[1].

CI-1040 also induces apoptosis and curtails proliferation in U-937 cells in a dose- and time-dependent manner, significantly elevating PUMA mRNA and protein levels, which are markers of apoptotic processes[2].

CI-1040 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
23132-87 Growth Inhibition Assay IC50=5.16872 μM SANGER
639-V Growth Inhibition Assay IC50=9.64388 μM SANGER
647-V Growth Inhibition Assay IC50=49.3414 μM SANGER
697 Growth Inhibition Assay IC50=3.69603 μM SANGER

CI-1040 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00034827 Colorectal Neoplasms ... 展开 >> Breast Neoplasms Carcinoma, Non-Small-Cell Lung Pancreatic Neoplasms 收起 << Phase 2 Completed - United States, Alabama ... 展开 >> Pfizer Investigational Site Birmingham, Alabama, United States, 35205 Pfizer Investigational Site Birmingham, Alabama, United States, 35233 United States, California Pfizer Investigational Site Blendora, California, United States, 91740 Pfizer Investigational Site Glendale, California, United States, 91204 Pfizer Investigational Site Huntington Beach, California, United States, 92648 Pfizer Investigational Site Long Beach, California, United States, 90813 Pfizer Investigational Site Los Alamitos, California, United States, 90720 Pfizer Investigational Site Los Angeles, California, United States, 90048 Pfizer Investigational Site Los Angeles, California, United States, 90095 Pfizer Investigational Site Mission Hills, California, United States, 91345 Pfizer Investigational Site Northridge, California, United States, 91328 Pfizer Investigational Site Oxnard, California, United States, 93030 Pfizer Investigational Site Pasadena, California, United States, 91105 Pfizer Investigational Site Pomona, California, United States, 91767 Pfizer Investigational Site Rancho Cucamonga, California, United States, 91730 Pfizer Investigational Site Redondo Beach, California, United States, 90277 Pfizer Investigational Site Santa Monica, California, United States, 90404 Pfizer Investigational Site Torrance, California, United States, 90505 Pfizer Investigational Site Ventura, California, United States, 93003 Pfizer Investigational Site West Covina, California, United States, 91790 United States, Georgia Pfizer Investigational Site Atlanta, Georgia, United States, 30342 Pfizer Investigational Site Decatur, Georgia, United States, 30033 Pfizer Investigational Site Macon, Georgia, United States, 30342 United States, Kentucky Pfizer Investigational Site Crestview Hills, Kentucky, United States, 41017 United States, Michigan Pfizer Investigational Site Detroit, Michigan, United States, 48201 United States, Minnesota Pfizer Investigational Site Rochester, Minnesota, United States, 55905 United States, Ohio Pfizer Investigational Site Cincinnait, Ohio, United States, 45236 Pfizer Investigational Site Cincinnati, Ohio, United States, 45219 Pfizer Investigational Site Cincinnati, Ohio, United States, 45230 Pfizer Investigational Site Cincinnati, Ohio, United States, 45242 收起 <<
NCT00033384 Breast Cancer ... 展开 >> Colorectal Cancer Lung Cancer Pancreatic Cancer 收起 << Phase 2 Completed - United States, Alabama ... 展开 >> University of Alabama at Birmingham Comprehensive Cancer Center Birmingham, Alabama, United States, 35294-3300 收起 <<

CI-1040 参考文献

[1]Allen LF, et al. CI-1040 (PD184352), a targeted signal transduction inhibitor of MEK (MAPKK). Semin Oncol. 2003 Oct;30(5 Suppl 16):105-16.

[2]Wei CR, et al. MEK inhibitor CI-1040 induces apoptosis in acute myeloid leukemia cells in vitro. Eur Rev Med Pharmacol Sci. 2016 May;20(10):1961-8.

[3]Kramer BW, et al. Use of mitogenic cascade blockers for treatment of C-Raf induced lung adenoma in vivo: CI-1040strongly reduces growth and improves lung structure. BMC Cancer. 2004 Jun 1;4:24.

CI-1040 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.45mL

2.09mL

1.04mL

20.89mL

4.18mL

2.09mL

CI-1040 技术信息

CAS号212631-79-3
分子式C17H14ClF2IN2O2
分子量 478.66
别名 PD 184352
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度

DMSO: 105 mg/mL(219.36 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: CI-1040 | 212631-79-3 | PD 184352 | CI1040 | CI 1040 | PD184352 | PD-184352 | MEK Inhibitor | MAPK/ERK Pathway | Apoptosis | MEK | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | CI-1040 纯度/质量文件 | CI-1040 亚型比较 | CI-1040 生物活性 | CI-1040 细胞研究 | CI-1040 临床数据 | CI-1040 参考文献 | CI-1040 实验方案 | CI-1040 技术信息

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