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网站主页 化工产品目录 生物化工 抑制剂 丝裂原活化蛋白激酶(MAPK) MEK 抑制剂 N-[(2R)-2,3-二羟基丙氧基]-3,4-二氟-2-[(2-氟-4-碘苯)氨基]苯甲酰胺 化合物 PD0325901
  • 化合物 PD0325901|T6189

化合物 PD0325901|T6189

Mirdametinib
391210-10-9
￥189 1mg 起订
￥428 5mg 起订
￥738 10mg 起订
上海 更新日期：2024-09-15

TargetMol中国（陶术生物）

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产品详情:

中文名称：
化合物 PD0325901
英文名称：
Mirdametinib
CAS号：
391210-10-9
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.63%
产品类别：
抑制剂
货号：
T6189

Product Introduction

Bioactivity

名称Mirdametinib
描述Mirdametinib (PD325901) is an MEK inhibitor (IC50=0.33 nM) with selective, non-ATP-competitive, and oral activity. Mirdametinib exhibits antitumor activity by inhibiting p-ERK1/2 expression and inducing apoptosis.
细胞实验A cell death detection enzyme-linked immunosorbent assay was used per the manufacturer's instructions. Briefly, 4 × 10^4 cells were plated in 24-well plates in triplicate the day before treatment. PTC cells were treated with 0.1 μmol/L PD0325901 for 96 hours. Cells treated with 1 μmol/L staurosporine served as positive controls for apoptosis. At the end of treatment, cells were lysed using the lysis buffer provided in the kit for 30 minutes at room temperature and then centrifuged in 24-well plates. Lysates (20 μL of supernatant) were transferred to streptavidin-coated wells and incubated for 2 hours at room temperature with two antibodies (biotin-labeled anti-histone antibody and peroxidase-conjugated anti-DNA antibody). After the wells were washed three times, the samples were incubated with peroxidase substrate (ABTS) and the amount of colored product was determined spectrophotometrically at 405 nm. The background was measured at 490 nm [2].
激酶实验Incorporation of 32P into myelin basic protein (MBP) is assayed in the presence of a glutathione S-transferase fusion protein containing p44MAP kinase (GST-MAPK) and a glutathione S-transferase protein containing p45MEK (GST-MEK). The assay solution contained 20 mM HEPES, pH 7.4, 10 mM MgCl2, 1 mM MnCl2, 1 mM EGTA, 50 mM [γ-32P]ATP, 10 mg GST-MEK, 0.5 mg GST-MAPK and 40 mg MBP in a final volume of 100 mL. Reactions are stopped after 20 minutes by addition of trichloroacetic acid and filtered through a GF/C filter mat. 32P retained on the filter mat is determined using a 1205 Betaplate [1].
动物实验Athymic Ncr-nu/nu mice were obtained from the National Cancer Institute at ages 6 to 8 weeks and housed for at least 1 week after arrival. Mice (10–14 per group) were anesthetized s.c. with a cocktail (100 μL/10 g body weight of 10 mg/mL ketamine and 1 mg/mL xylazine). K2 and TPC-1 cells stably infected with a retrovirus expressing luciferase (5 × 105 cells in 5 μL RPMI1640 medium) were inoculated into the thyroid gland, and the mice were monitored weekly for tumor growth by Xenogen (IVIS 200 imaging system) using Living Image 3.0 software. One week after inoculation, PD0325901 was dissolved in 80 mmol/L citric buffer (pH 7) by sonication and given to mice daily by oral gavage (20–25 mg/kg) for 3 weeks (5 consecutive days/week). Mice were sacrificed only due to tumor burden or loss of 20% of body weight. Tumor sizes were measured with calipers and tumor volume (V) was calculated by the formula (V = length × width × depth). Control mice were given 80 mmol/L citric buffer (pH 7) alone. All in vivo experiments were done at least twice [2].
体外活性方法：11 种人黑色素瘤细胞系上用 Mirdametinib (0.1-1000 nM) 处理 72 h，使用 trypan blue exclusion test 检测细胞数。 结果：Mirdametinib (IC50=20-50 nM) 有效抑制具有 BRAF 突变 (M14/A375P/A375M/A375SM/ME10538/ME4686/JR8) 或不具有 BRAF 突变 (ME4405/ME13923) 的人黑色素瘤细胞系的生长。ME1007 和 ME8959均具有野生型 BRAF，对 Mirdametinib介导的生长抑制的抗性略高 (IC50≥100 nM)。[1] 方法：乳头状甲状腺癌 (PTC) 细胞系 K2 和 TPC-1 用 Mirdametinib (0.1-1000 nmol/L) 处理 1-96 h，使用 Western Blot 检测靶点蛋白表达水平。 结果：Mirdametinib 可以有效抑制多种 PTC 细胞系中 ERK1/2 的磷酸化。[2]
体内活性方法：为检测体内抗肿瘤活性，将 Mirdametinib (20-25 mg/kg，80 mmol/L citric buffer (pH 7)) 灌胃给药给携带 PTC 肿瘤 K2 或 TPC-1 的 Athymic Ncr-nu/nu 小鼠，每周五次，持续三周。 结果：Mirdametinib 在接种携带 BRAF 突变的 PTC 细胞 K2 的小鼠中完全抑制肿瘤生长，并且在接种携带 RET/PTC1 重排的 PTC 细胞 TPC-1 的小鼠中显着降低肿瘤生长。[2] 方法：为检测体内抗肿瘤活性，将 Mirdametinib (1.6-25 mg/kg，0.5% hydroxypropylmethylcellulose+0.2% Tween 80 in water) 口服给药给携带小鼠结直肠癌肿瘤 CT26 的小鼠，每天一次，持续十四天。 结果：Mirdametinib 显著抑制肿瘤中的 pERK 水平。[3]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (10.37 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
H2O : Insoluble
DMSO : 50 mg/mL (103.69 mM)
关键字PD 0325901 | MAPKK | Mitogen-activated protein kinase kinase | Apoptosis | MEK | PD-0325901 | Autophagy | inhibit | MAP2K | PD-325901 | Inhibitor | PD 325901 | Mirdametinib
相关产品Guanidine hydrochloride | Naringin | Valproic Acid | L-Glutamic acid | Gefitinib | Hydroxychloroquine | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | L-Ascorbic acid | Paeonol | Sodium 4-phenylbutyrate
相关库抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 已知活性化合物库 | 高选择性抑制剂库 | 抗衰老化合物库 | 疼痛相关化合物库 | 酪氨酸激酶分子库 | 抗癌临床化合物库 | 抗癌药物库
PD325901|||PD0325901|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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