PD0325901
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
PD0325901是一种特异性的MEK（mitogen-activated protein kinase kinase）小分子抑制剂，其分子式为C16H14F3IN2O4，分子量为482。MEK是RAS/RAF/MEK/ERK信号通路的关键组成部分，该信号通路在人类肿瘤中频繁被激活。MEK/ERK调控细胞外信号刺激的细胞增殖、存活和分化。在体外，PD0325901有效减少P-ERK的水平。在小鼠模型中，PD0325901抑制肿瘤生长。
参考文献：
1. Noninvasive imaging of cell proliferation following mitogenic extracellular kinase inhibition by PD0325901. J Leyton, G Smith, M Lees, M Peruma. Molecular cancer Therapeutics. 2008
2. Targeting mitogen‐activated protein kinase kinase with the inhibitor PD0325901 decreases hepatocellular carcinoma growth in vitro and in mouse model. M Hennig, MT Yip‐Schneider, S Wentz, H Wu. Hepatology. 2010
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| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 482.19 |
| Cas No. | 391210-10-9 |
| Formula | C16H14F3IN2O4 |
| Synonyms | PD0325901,PD-0325901,PD 0325901,PD325901,PD 325901,PD-325901 |
| Solubility | ≥24.1 mg/mL in DMSO; insoluble in H2O; ≥55.4 mg/mL in EtOH |
| Chemical Name | N-[(2R)-2,3-dihydroxypropoxy]-3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzamide |
| SDF | Download SDF |
| Canonical SMILES | C1=CC(=C(C=C1I)F)NC2=C(C=CC(=C2F)F)C(=O)NOCC(CO)O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
|
细胞系 |
M14（BRAFV600E）细胞 |
|
溶解方法 |
在DMSO中的溶解度 >10 mM。为了获得更高的浓度，可以将离心管在37°C加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20°C以下储存几个月。 |
|
反应条件 |
细胞周期积累：1 μM，48 h；DNA减少：≥100 nM，72 h |
|
应用 |
PD0325901引起剂量和时间依赖的G1/S期细胞周期积累和S期细胞的耗竭，也引起剂量和时间依赖的含亚G1 DNA含量的细胞百分比的增加，表明细胞凋亡的诱导。与细胞周期抑制的动力学和剂量-反应曲线相比较，DNA减少到亚G1水平需要更长时间（72小时）的暴露和更高的药物浓度（≥100 nM）。 |
| 动物实验[1]： | |
|
动物模型 |
植入M14（BRAFV600E）和ME8959（wtBRAF）细胞的雌性CD-1裸（nu/nu）鼠。 |
|
剂量 |
50 mg/kg/day，21天；口服给药 |
|
应用 |
在建立的M14和ME8959异种移植肿瘤模型中，每日口服50 mg/kg的PD0325901，在21天的治疗结束后，与对照相比，PD0325901显著抑制60%-65%的肿瘤生长。PD0325901的效应是可逆的，在治疗中断后肿瘤重新开始生长。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Ciuffreda L, Del Bufalo D, Desideri M, et al. Growth-inhibitory and antiangiogenic activity of the MEK inhibitor PD0325901 in malignant melanoma with or without BRAF mutations. Neoplasia, 2009, 11(8): 720-W6. |
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| Targets | ||||||
| IC50 |
质量控制和MSDS
- 批次:
化学结构
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