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- CAS号：
212631-79-3
- 规格：
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥392.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥174.0 |
| 规格： | 5mg | 产品价格： | ￥354.0 |
| 规格： | 10mg | 产品价格： | ￥596.0 |
| 规格： | 25mg | 产品价格： | ￥1192.0 |
| 规格： | 50mg | 产品价格： | ￥1856.0 |
| 规格： | 100mg | 产品价格： | ￥3112.0 |
| 规格： | 200mg | 产品价格： | ￥3912.0 |
Product Introduction
Bioactivity
| 名称 | CI-1040 |
| 描述 | CI-1040 (PD 184352) (PD184352) is an ATP non-competitive MEK1/2 inhibitor (IC50: 17 nM). |
| 细胞实验 | Cells were planted seeded in T-75 cm2 flasks and treated the next day for 24 h with either DMSO or PD 184352. Single-cell suspensions were collected, and pellets were fixed in ice-cold ethanol (70%) for 30 min. After centrifugation of the samples, propidium iodide (50 μg/ml) and RNase (30 units/ml) were added to the pellets for 20 min at 37 °C. After filtration, samples were analyzed by flow cytometry [1]. |
| 激酶实验 | All protein kinase activities were linear with respect to time in every incubation. Assays were performed either manually for 10 min at 30 °C in 50 μl incubations using [γ-32P]ATP, or with a Biomek 2000 Laboratory Automation Workstation in a 96-well format for 40 min at ambient temperature in 25 μl incubations using [γ-33P]ATP. The concentrations of ATP and magnesium acetate were 0.1 mM and 10 mM respectively, unless stated otherwise. This concentration of ATP is 5–10-fold higher than the Km for ATP of most of the protein kinases studied in the present paper, but lower than the normal intracellular concentration, which is in the millimolar range. All assays were initiated with MgATP. Manual assays were terminated by spotting aliquots of each incubation on to phosphocellulose paper, followed by immersion in 50 mM phosphoric acid. Robotic assays were terminated by the addition of 5 μl of 0.5 M phosphoric acid before spotting aliquots on to P30 filter mats. All papers were then washed four times in 50 mM phosphoric acid to remove ATP, once in acetone (manual incubations) or methanol (robotic incubations), and then dried and counted for radioactivity [2]. |
| 动物实验 | Tumor fragments (approximately 3 mm^3 in size) were implanted subcutaneously into the right axillae of CD2F1 male mice (colon 26 studies) or female nude mice (HT-29 studies) 4–6 weeks old. Treatment was administered by gavage or intraperitoneally and was initiated either the day after tumor implantation (colon 26) or when tumors reached approximately 200 mg in size (HT-29). PD 184352 was prepared in a vehicle of 10% Cremophore EL, 10% ethanol and 80% water. Tumor size was evaluated periodically by caliper measurements, generally three times per week. Percent tumor growth inhibition was calculated as [(T–C)/number of days of treatment] × 100, with T and C being defined as the time required for treated and control tumors, respectively, to reach 750 mg (colon 26) or to reach twofold growth (HT-29) [1]. |
| 体外活性 | PD 184352（CI-1040）显著降低了在血清存在条件下生长的多种肿瘤细胞系中磷酸化MAPK（pMAPK）的稳态水平。在含1 μM PD 184352 的培养基中处理结肠26细胞1小时，可使pMAPK水平降低超过75%。用10 μM PD 184352处理结肠26细胞，不会抑制Jun激酶、p38激酶或AKT的磷酸化[1]。PD 184352抑制MKK1的IC50为0.3 μM，这比抑制Swiss 3T3细胞中EGF诱导的ERK2活化所需浓度高出15倍。在2 nM PD 184352 的作用下，MKK1在细胞中的活化被50%抑制[2]。CI-1040以剂量和时间依赖的方式诱导U-937细胞凋亡和抑制增殖。CI-1040显著增加PUMA mRNA和蛋白水平。通过PUMA siRNA转染敲低PUMA，可以抑制CI-1040诱导的U-937细胞凋亡和增殖抑制[3]。 |
| 体内活性 | 处理PD 184352（150 mg/kg，i.p. 或 p.o.）后1小时和6小时切除了肿瘤。无论通过何种给药方式，PD 184352处理至少6小时内完全抑制了MAPK磷酸化。MAPK磷酸化在给药后12小时恢复，并在24小时达到对照水平[1]。体内，MEK抑制剂CI-1040的系统给药将腺瘤形成减少至三分之一，并显著恢复了肺结构。CL-1040处理的小鼠肺细胞的增殖率降低，对肺泡细胞的分化没有明显影响[4]。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : < 10 mg/mL (20.89 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+90% (20% SBE-β-CD in Saline) : < 10 mg/mL (20.89 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+90% Saline : < 10 mg/mL (20.89 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. Ethanol : 12 mg/mL (25.07 mM), Sonication is recommended. DMSO : 125 mg/mL (261.15 mM), Sonication is recommended. 10% DMSO+90% Corn oil : 10 mg/mL (20.89 mM), Solution. |
| 关键字 | PD-184352 | PD184352 | Mitogen-activated protein kinase kinase | MEK2 | MEK1 | MEK | MAPKK | MAP2K | Inhibitor | inhibit | CI-1040 | CI1040 | CI 1040 | Apoptosis |
| 相关产品 | Formamide | Urea | Sodium Molybdate | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Tamoxifen |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Highly Selective Inhibitor Library | Clinical Compound Library | Immunology/Inflammation Compound Library | Pain-Related Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 CI-1040【212631-79-3】
￥174 - 3912
