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PD 184161 Sale

目录号 : GC15646

A potent MEK1/2 inhibitor

PD 184161 Chemical Structure

Cas No.:212631-67-9

规格 价格 库存 购买数量
1mg
¥214.00
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5mg
¥918.00
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10mg
¥1,632.00
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25mg
¥3,569.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

IC50: 10-100 nM

PD 184161 is a MEK1/2 inhibitor.

The intracellular signaling pathway of mitogen-activated protein kinases is involved in the regulation of various cellular functions. One of these pathways, named Raf/MEK/ERK pathway, plays a key role in the regulation of cellular differentiation, growth, and proliferation. The modulation of this Raf/MEK/ERK pathway has been reported as a useful approach to treate proliferative disorders such as cancer.

In vitro: Previous study found that PD184161 could inhibit MEK activity in a time- and concentration-dependent manner, which was more effectively than PD098059 or U0126. Moreover, PD184161 could inhibit cell proliferation and induce apoptosis at concentrations of > or = 1.0 μM time- and concentration-dependently [1].

In vivo: Animal study showd that tumor xenograft P-ERK levels were significantly reduced 3 to 12 hours after an oral dose of PD184161. Contrarily, tumor xenograft P-ERK levels following long-term treatment of PD184161 were refractory to this signaling effect. PD184161 also significantly suppressed tumor engraftment and initial growth, however, established tumors were not significantly affected. In summary, PD184161 has antitumor effects in HCC in vivo that appear to correlate with suppression of MEK activity [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Klein, P. J.,Schmidt, C.M.,Wiesenauer, C.A., et al. The effects of a novel MEK inhibitor PD184161 on MEK-ERK signaling and growth in human liver cancer. Neoplasia 8(1), 1-8 (2006).

Chemical Properties

Cas No. 212631-67-9 SDF
化学名 5-bromo-2-[(2-chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluoro-benzamide
Canonical SMILES FC1=C(NC2=C(Cl)C=C(I)C=C2)C(C(NOCC3CC3)=O)=CC(Br)=C1F
分子式 C17H13BrClF2IN2O2 分子量 557.6
溶解度 ≤10mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide 储存条件 Store at -20°C
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储备液的保存方式和期限:-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。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.7934 mL 8.967 mL 17.934 mL
5 mM 0.3587 mL 1.7934 mL 3.5868 mL
10 mM 0.1793 mL 0.8967 mL 1.7934 mL
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