曲美替尼|T2125

Trametinib
871700-17-3

￥282 10瓶起订

￥2537 500瓶起订

￥452 25瓶起订

￥320 1瓶起订

￥1050 100瓶起订

￥654 50瓶起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 曲美替尼

英文名称：: Trametinib

CAS号：: 871700-17-3

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：: 99.88%

产品类别：: 抑制剂

货号：: T2125

Product Introduction

Bioactivity

名称	Trametinib
描述	Trametinib (GSK1120212) is a MEK inhibitor that inhibits MEK1 and MEK2 (IC50=0.7/0.9 nM) with ATP non-competitive and oral activity. Trametinib activates autophagy and induces apoptosis.
细胞实验	These cells were maintained in media recommended by the providers. Exponentially growing cells were precultured in 96-well tissue culture plates for 24 h and then exposed to JTP-74057. Cell growth was determined by an in vitro toxicology assay kit, sulforhodamine B based. For combination studies, two compounds were simultaneously added to the HT-29 cells and incubated for 72 h. In the presence of various concentrations of compound A, the 50% inhibitory concentration (IC50) values of compound B were determined. Then, the fixed concentration of compound A versus the IC50 value of compound B was plotted. Conversely, the IC50 values of compound A were determined in the presence of various concentrations of compound B and plotted [1].
激酶实验	A Raf-MEK-ERK cascade kinase assay was carried out as previously described. Briefly, nonphosphorylated myelin basic protein (MBP) was coated onto an ELISA plate, and the active form of B-Raf/c-Raf was mixed with unphosphorylated MEK1/MEK2 and ERK2 in 10 μM ATP and 12.5 mM MgCl2 containing MOPS buffer in the presence of various concentrations of JTP-74057. The phosphorylation of MBP was detected by the anti-phosphoMBP antibody. Kinase inhibitory activities against a total of 99 kinases were tested by kinase profiler at 10 μM ATP [1].
动物实验	Female BALB/c-nu/nu mice were used. On day 0, HT-29 cells or COLO205 cells suspended in ice-cold HBSS (-) were inoculated subcutaneously into the right flank of the mice at 5x10^6 cells/100 μl/site or 1x10^6 cells/100 μl/site, respectively. The acetic acid-solvated form of JTP-74057 was dissolved in 10% Cremophor EL-10% PEG400 and was administered orally once daily for 14 days from the day when the mean tumor volume reached 100 mm^3. The tumor length [L (mm)] and width [W (mm)] were measured using a micro gauge twice a week after the commencement of dosing, and the tumor volume was calculated using the following formula: tumor volume (mm^3) = L x W x W/2. All procedures relating to the use of animals in this study were reviewed and approved by the Institutional Animal Care and Use Committee of Japan Tobacco [1].
体外活性	方法：小鼠肝内胆管癌细胞 SB1、LD-1 和人肝内胆管癌细胞 EGI-1 用 Trametinib (0-10000 nM) 处理 48 h，使用 MTT 方法检测细胞生长抑制情况。结果：Trametinib 剂量依赖抑制 SB1、LD-1 和 EGI-1 细胞生长，IC50 分别为 41.48 nM、56.10 nM 和 27.89 nM。[1] 方法：人结肠癌细胞 RKO 用 Trametinib (200 nmol/L) 处理 30 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：Trametinib 显著降低 p-ERK 和 p-AKT 水平。[2] 方法：人胶质瘤细胞 U87 和 U251 用 Trametinib (50 nM) 孵育 6-72 h，使用 Flow Cytometry 方法检测细胞凋亡情况。结果：Trametinib 诱导 U87 和 U251 细胞的凋亡率明显增加。Trametinib 可以诱导神经胶质瘤细胞的晚期凋亡，而不会发生早期凋亡。[3]
体内活性	方法：为检测体内抗肿瘤活性，将 Trametinib (0.3-1 mg/kg) 口服给药给携带人结直肠癌肿瘤 HT-29 和 COLO205 的 BALB/c-nu/nu 小鼠，每天一次，持续十四天。结果：Trametinib 治疗显著抑制人结直肠癌肿瘤的生长，表明在体内具有抗肿瘤活性。[4] 方法：为检测体内抗肿瘤活性，将 Trametinib (5 mg/kg) 腹腔注射给携带人B淋巴细胞白血病肿瘤 KOPN8 和 COLO205 的 NSG 小鼠，每周三次，持续十四天。结果：Trametinib 单药治疗延缓了白血病的进展，但不足以防止白血病的生长。[5]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 7.86 mg/mL (12.77 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字	inhibit \| MAP2K \| Apoptosis \| Autophagy \| Inhibitor \| Trametinib \| orally \| type \| MAPKK \| collageninduced \| MEK \| arthritis \| AIA \| GSK 1120212 \| JTP74057 \| Mitogen-activated protein kinase kinase \| GSK-1120212 \| Adjuvant-induced \| JTP 74057 \| CIA
相关产品	Guanidine hydrochloride \| Naringin \| Gefitinib \| Hydroxychloroquine \| Stavudine \| L-Ascorbic acid \| Paeonol \| Sodium 4-phenylbutyrate
相关库	经典已知活性库 \| 抗癌上市药物库 \| 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 \| 神经退行性疾病化合物库 \| 酪氨酸激酶分子库 \| 药物功能重定位化合物库 \| 疼痛相关化合物库

GSK1120212|||JTP-74057|||曲美替尼

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