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 activeMEKinhibitor. PD184161 inhibitsMEKactivity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and inducesapoptosis. PD184161 produces depressive-like behavior[1][2]. |
| IC50& Target[1] | |
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].
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. |
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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].
| 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. |
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| 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 | 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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 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本网站选购。
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