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PD0325901MEK抑制剂

PD0325901

产品编号:A3013
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规格 单价 库存 订购数量
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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Sample solution is provided at 25 µL, 10mM.

引用文献

1. Sima J, Chakraborty A, et al. "Identifying cis Elements for Spatiotemporal Control of Mammalian DNA Replication." Cell. 2019 Feb 7;176(4):816-830.e18. PMID:30595451
2. Wang Y, Li Y, et al. "The cerebral cavernous malformation disease causing gene KRIT1 participates in intestinal epithelial barrier maintenance and regulation." FASEB J. 2018 Sep 25:fj201800343R. PMID:30252535
3. Kopanitsa MV, Gou G, et al. "Chronic treatment with a MEK inhibitor reverses enhanced excitatory field potentials in Syngap1(+/-) mice." Pharmacol Rep. 2018 Jun 22;70(4):777-783. PMID:29940508
4. Potonjak I, Gobin I, et al. "Carvacrol induces cytotoxicity in human cervical cancer cells but causes cisplatin resistance: Involvement of MEK-ERK activation." Phytother Res. 2018 Feb 8. PMID:29417642
5. Sieber J, Wieder N, et al. "GDC-0879, a BRAF(V600E) Inhibitor, Protects Kidney Podocytes from Death." Cell Chem Biol. 2017 Dec 6. PMID:29249695

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

PD0325901 Dilution Calculator

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化学性质

CAS号 391210-10-9 SDF Download SDF
别名 PD0325901,PD-0325901,PD 0325901,PD325901,PD 325901,PD-325901
化学名 N-[(2R)-2,3-dihydroxypropoxy]-3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzamide
SMILES C1=CC(=C(C=C1I)F)NC2=C(C=CC(=C2F)F)C(=O)NOCC(CO)O
分子式 C16H14F3IN2O4 分子量 482.19
溶解度 ≥24.1mg/mL in DMSO 储存条件 Store at -20°C
物理性状 A solid 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。

生物活性

Targets            
IC50            

实验操作

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.

研究更新

1. Modulation of endochondral ossification by MEK inhibitors PD 0325901 and AZD6244 (Selumetinib). Bone. 2014 Feb;59:151-61. doi: 10.1016/j.bone.2013.11.013. Epub 2013 Nov 20.
Abstract
PD 0325901, a MEKi, affects chondrocyte hypertrophy, matrix resorption, fracture healing and bone architecture, where it expands the hypertrophic zone of th growth plate and reduces osteoclast surface systemically.
4. MEK inhibitor PD0325901 significantly reduces the growth of papillary thyroid carcinoma cells in vitro and in vivo. Mol Cancer Ther. 2010 Jul;9(7):1968-76. doi: 10.1158/1535-7163.MCT-10-0062. Epub 2010 Jun 29.
Abstract
PD0325901, a MEK1/2 inhibitor, is an effective drug for the treatment of thyroid cancers with RET/PTC or BRAF mutation, where PTC cells with a BRAF mutation is more sensitive to PD0325901 than PTC cells with RET/PTC1 rearrangement.
5. Targeting mitogen-activated protein kinase kinase with the inhibitor PD0325901 decreases hepatocellular carcinoma growth in vitro and in mouse model systems. Hepatology. 2010 Apr;51(4):1218-25. doi: 10.1002/hep.23470.
Abstract
PD0325901, a MEK inhibitor with possible inhibitory effects against HCC tumorigenesis, inhibited tumor growth and MEK activity in various HCC cells and HCC mouse models.

产品描述

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