PD184161|cas:212631-67-9|西域试剂

PD184161,99.38%

产品编号：Bellancom-10174| CAS NO：212631-67-9| 分子式：C₁₇H₁₃BrClF₂IN₂O₂| 分子量：557.56

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-10174	￥900.00	杭州北京（现货）
Bellancom-10174	￥1600.00	杭州北京（现货）
Bellancom-10174	￥3500.00	杭州北京（现货）
Bellancom-10174	￥5800.00	杭州北京（现货）
Bellancom-10174	￥9200.00	杭州北京（现货）

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PD184161

产品介绍

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。

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.

体外研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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

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

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

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.
PD184161 (300 mg/kg; orogastric gavage twice daily for 38 days) significantly suppresses tumor engraftment and initial growth.
PD184161 (30 mg/kg; i.p.; single injection) produces depressive-like behavior.
PD184161 (500 μg/kg; intravenous injection) prevents the progression of neurological deficits and brain damage after stroke.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Hep3B tumor xenografts BALB/c athymic nude mice
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
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
Dosage:	30 mg/kg
Administration:	i.p., single injection
Result:	Produced depressive-like behavior.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Hep3B tumor xenografts BALB/c athymic nude mice
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
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
Dosage:	30 mg/kg
Administration:	i.p., single injection
Result:	Produced depressive-like behavior.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Hep3B tumor xenografts BALB/c athymic nude mice
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
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
Dosage:	30 mg/kg
Administration:	i.p., single injection
Result:	Produced depressive-like behavior.

性状

Solid

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。