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PD0325901

现货
Catalog No.
A3013
MEK抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
5mg
¥ 450.00
现货
25mg
¥ 1,500.00
现货
100mg
¥ 3,600.00
现货
500mg
¥ 9,800.00
现货

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Background

PD0325901 is a specific inhibitor of mitogen-activated protein kinase MEK. PD0325901 is a small molecular with the formula of C16H14F3IN2O4 and Molecular Weight of 482. MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors, and MEK/ERK regulates cell proliferation, survival, and differentiation in response to extracellular signals. PD0325901 effectively reduces P-ERK levels and cell growth in vitro, and inhibits tumor growth in mouse model in vivo

References:
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

文献引用

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt482.19
Cas No.391210-10-9
FormulaC16H14F3IN2O4
SynonymsPD0325901,PD-0325901,PD 0325901,PD325901,PD 325901,PD-325901
Solubility≥24.1mg/mL in DMSO
Chemical NameN-[(2R)-2,3-dihydroxypropoxy]-3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzamide
SDFDownload SDF
Canonical SMILESC1=CC(=C(C=C1I)F)NC2=C(C=CC(=C2F)F)C(=O)NOCC(CO)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

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℃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℃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.

生物活性

Targets            
IC50            

质量控制

化学结构

PD0325901

相关生物数据

PD0325901
Inhibition of the PI3K and MEK-ERK pathway enhances cell death in HCT116 cells. HCT116 cells stably transduced with control or PIK3CA inducible shRNA were treated with PD0325901 in the presence or absence of doxycycline. HCT116 cells grown in the presence or absence of doxycycline were treated with PD0325901 for 48 h. Cells were subsequently fixed with formaldehyde and stained with Hoechst 33342 to visualize fragmented nuclei. For each treatment condition, 1,500 cells were counted under a fluorescence microscope.

相关生物数据

PD0325901

相关生物数据

PD0325901

相关生物数据

PD0325901