PD184161

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PD184161  纯度: 99.38%

PD184161 是一种口服有效、时间和浓度依赖的 MEK 抑制剂 (IC50=10-100 nM)。PD184161 抑制细胞增殖并诱导细胞凋亡 (apoptosis)。PD184161 诱导抑郁样行为。

PD184161

PD184161 Chemical Structure

CAS No. : 212631-67-9

规格 价格 是否有货 数量
5 mg ￥900 In-stock
10 mg ￥1600 In-stock
25 mg ￥3500 In-stock
50 mg ￥5800 In-stock
100 mg ￥9200 In-stock
200 mg   询价  
500 mg   询价  

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PD184161 相关产品

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生物活性

PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior[1][2].

IC50 & Target[1]

MEK

10-100 nM (IC50)

体外研究
(In Vitro)

PD184161 (1-20 μM; 24, 48, or 72 hours) inhibits cell proliferation and induces apoptosis in a time and concentration dependent manner[1].
PD184161 (0.1 and 1.0 μM; 1 hour) inhibits ERK1,2 phosphorylation[1].
PD184161 (5 μM; 30 min) prevents the toxic effects of bicuculline[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: HCC cell lines (HepG2, Hep3B, PLC, and SKHep)
Concentration: 1-20 μM
Incubation Time: 24, 48, or 72 hours
Result: Inhibited cell proliferation.

Apoptosis Analysis[1]

Cell Line: HCC cell lines (HepG2, Hep3B, PLC, and SKHep)
Concentration: 1-20 μM
Incubation Time: 48 hours
Result: Induced cell apoptosis.

Western Blot Analysis[1]

Cell Line: HCC cell lines (HepG2, Hep3B, PLC, and SKHep)
Concentration: 0.1 and 1.0 μM
Incubation Time: 1 hours
Result: Inhibited ERK1,2 phosphorylation.

Cell Viability Assay[3]

Cell Line: Primary mouse neurons
Concentration: 5 μM
Incubation Time: 30 min
Result: Prevents the toxic effects of bicuculline.

体内研究
(In Vivo)

PD184161 reduces tumor xenograft P-ERK levels in 3-12 hours after an oral dose[1].
PD184161 (300 mg/kg; orogastric gavage twice daily for 38 days) significantly suppresses tumor engraftment and initial growth[1].
PD184161 (30 mg/kg; i.p.; single injection) produces depressive-like behavior[2].
PD184161 (500 μg/kg; intravenous injection) prevents the progression of neurological deficits and brain damage after stroke[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Hep3B tumor xenografts BALB/c athymic nude mice[1]
Dosage: 300 mg/kg
Administration: Orogastric gavage twice daily for 38 days
Result: Decreased the early tumor growth.
Animal Model: Male, 6 weeks C57Bl/6 mice[2]
Dosage: 500 μg/kg
Administration: intravenously in 30 min before MCAO or PTZ administration
Result: Prevented the progression of neurological deficits and brain damage after stroke.
Animal Model: C57Bl/6 mice[3]
Dosage: 30 mg/kg
Administration: i.p., single injection
Result: Produced depressive-like behavior.

分子量

557.56

Formula

C17H13BrClF2IN2O2
CAS 号

212631-67-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (179.35 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7935 mL 8.9676 mL 17.9353 mL
5 mM 0.3587 mL 1.7935 mL 3.5871 mL
10 mM 0.1794 mL 0.8968 mL 1.7935 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (4.48 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.48 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.48 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.48 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Klein PJ, et al. The effects of a novel MEK inhibitor PD184161 on MEK-ERK signaling and growth in human liver cancer. Neoplasia. 2006 Jan;8(1):1-8.

    [2]. Duman CH, et al. A role for MAP kinase signaling in behavioral models of depression and antidepressant treatment. Biol Psychiatry. 2007 Mar 1;61(5):661-70.

    [3]. Gladbach A, et al. ERK inhibition with PD184161 mitigates brain damage in a mouse model of stroke. J Neural Transm (Vienna). 2014 May;121(5):543-7.

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