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PD98059
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PD98059图片
CAS NO:167869-21-8
包装:5mg, 10mg, 25mg, 100mg
包装与价格:
包装价格(元)
Free Sample (0.5-1 mg)电议
10mM*1mL in DMSO电议
5mg电议
10mg电议
25mg电议
100mg电议

产品名称
PD 98059
产品介绍

生物活性

PD98059是一种非ATP竞争性的MEK抑制剂,IC50为2 μM,特异性抑制MEK-1介导的MAPK激活;PD98059 是一种 ERK1/2 信号的抑制剂。PD98059 要么抑制本底的MEK1,要么抑制一种被部分激活的MEK突变体,该突变体是 218 和 222号位上丝氨酸突变为谷氨酸后形成的(MEK-2E), IC50 为2 μM. PD98059 不会抑制JNK和P38这两个 MAPK 的同系物. PD98059会高度选择性的抑制MEK, 因为对其它包括Raf 激酶, cAMP-依赖性激酶, 蛋白激酶C, v-Src, 表皮生长因子 (EGF) 受体激酶, 胰岛素受体激酶, PDGF 受体激酶, 和磷脂酰肌醇(-3)激酶等在内的一系列激酶都没有抑制性。 PD98059 会抑制经过PDGF刺激而活化的MAPK 和胸苷 进入 3T3 细胞, IC50分别为 ~10 μM 和 ~7 μM 。PD98059可以有效地阻止 MEK1 被Raf 或者MEK 激酶活化, IC50为4 μM, 可以微弱地 抑制MEK2被 Raf 活化, IC50 为50 μM。研究表明,PD98059抑制ERK信号通路后,细胞内KAT2B蛋白的表达显着降低,提示17β-E 2 可通过激活ERK信号通路增加KAT2B蛋白表达,从而增强ER活性,增强雌激素效应的正反馈。


化学数据

分子量267.28
分子式C16H13NO3
CAS号167869-21-8
纯度99.83%
溶解性(25°C)DMSO 15 mg/mL
储存和运输条件-20°C, dry, sealed, protect from light
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系C-33 and C-81 cells
方法Treatment with chemotherapeutic agents.
Cells were seeded in 6-well culture plates in regular culture medium at a density of 2.5*105 and 1*105 cells/well for C-33 and C-81 cells, respectively, for 2 days and then fed with SR medium, i.e., PR-free RPMI-1640 medium containing 5% heat-inactivated CS-FBS, 1% glutamine and 0.5% gentamicin. Two days after steroid starvation, one set of attached cells was harvested and counted as day 0. The remaining cells were fed with fresh SR medium and treated with PD98059, U0126, vinorelbine, docetaxel or various combinations in which the dosage of each reagent was specified. Control cells were maintained in SR medium and received solvent alone without chemotherapeutic agents. Fresh SR medium with or without chemotherapeutic agents was added every 3 days. Treatment was continued for 3 or 6 days, as described in each figure legend. To quantify the inhibition of cell growth, attached cells were trypsinized and the cells counted with a Coulter counter. The number of cells in control sets that received solvent alone was designated as 100% for comparison. All experiments were done in triplicate and repeated at least twice.
浓度0~10 μM
处理时间3 or 6 days

动物实验
动物模型acute lung injury in mice
配制DMSO, then diluted with saline
剂量10mg/kg
给药处理i. p.

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM3.7414 mL18.707 mL37.4139 mL
5 mM0.7483 mL3.7414 mL7.4828 mL
10 mM0.3741 mL1.8707 mL3.7414 mL