培利替尼|T2327|TargetMol

Pelitinib
257933-82-7

￥269 1mg 起订

￥611 5mg 起订

￥987 10mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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联系人：邵小姐

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产品详情:

中文名称：: 培利替尼

英文名称：: Pelitinib

CAS号：: 257933-82-7

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：: 99.86%

产品类别：: 抑制剂

货号：: T2327

Product Introduction

Bioactivity

名称	Pelitinib
描述	Pelitinib (EKB-569) (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
细胞实验	Cells are seeded in 96-well dishes, and after 2 hours, Pelitinib is added and incubated for 5 days. After incubation, the medium is removed from each well and fresh medium (150 μL) + 1 mg/mL MTT solution (50 μL) is added. After incubation for 2 hours at 37 °C, the medium is replaced with 150 μL DMSO, and absorbance at 540 nm in each well is determined. The IC50 is calculated by linear regression of the data. (Only for Reference)
激酶实验	Autophosphorylation of EGFR in cells: For experiments using cells in culture, A431 cells are treated with various concentrations of Pelitinib for 2.75 hours before co-incubation with 100 ng/mL EGF for 0.25 hour. Cells are washed twice with cold phosphate-buffered saline (PBS) before adding to lysis buffer (10 mM Tris, pH 7.5, 5 mM ethylenediamine tetra-acetic acid (EDTA), 150 mM NaCl, 1% Triton X-100, 1% Sodium deoxycholate, 0.1 % SDS, 1 mM PMSF, 10 mg/mL pepstatin A, 10 mg/mL leupeptin, 20 KIU/mL aprotinin, 2 mM sodium orthovanadate, and 100 mM sodium fluoride) for 20 minutes on ice, before immunoprecipitation and SDS-PAGE-immunoblotting. For immunoprecipitation, cultured cells are placed in cold lysis buffer and immediately homogenized on ice with a polytron with several pulses. The homogenate is first centrifuged at 2500 rpm (20 minutes, 4 °C) and then again at 14,000 rpm in a microcentrifuge (10 minutes, 4 °C). Supernatants (1000 μg protein) are incubated for 2 hours at 4 °C with 15 mL of EGFR polyclonal antibody. After 2 hours, 50 μL of protein G plus/protein A agarose beads is added and incubated with constant rotation for 2 hours at 4 °C. After washing with lysis buffer, beads are boiled for 2 minutes in Laemmli sample buffer. Proteins are then resolved by SDS-PAGE, transferred to immobilon membrane and probed overnight with an anti-phosphotyrosine antibody conjugated with horseradish peroxidase (HRP). Membranes are developed using the ECL reagent. Total EGFR protein is determined by stripping membranes and re-probing with receptor-specific antibodies. Quantitation of bands is done by densitometry, using ImageQuant software with a Molecular Dynamics laser transmittance scanner.
体外活性	在达EGFR的A431异种移植模型中,Pelitinib（10 mg/kg,p.o.）可有效抑制EGFR磷酸化,1 h内抑制90%,24 h后抑制率>50%.小鼠气道上皮细胞重构模型,可被病毒感染诱导,具有延迟但永久性转变为杯状细胞化生的特点,Pelitinib（20 mg/kg/day）可完全阻断纤毛细胞的增加和Clara细胞的减少,从而从3个方面校正上皮细胞重构,并明显抑制杯状细胞的发生.Pelitinib（20 mg/kg/day）抑制APCMin/+小鼠体内87%的肿瘤发生,与2倍剂量EKI-785（40 mg/kg/day）的作用接近,与体内活性较高一致. Pelitinib对体内气道上皮细胞中EGFR信号有选择性抑制效果.
体内活性	Pelitinib（75-500 nM）可特异性抑制AKT和ERK1/2的活化,而对NF-κB通路无影响。在正常人角质细胞中,Pelitinib也可有效抑制TGF-α介导的EGFR活化（IC50：56 nM）,抑制STAT3和ERK1/2的活化（IC50：60 nM和62 nM）。在A431和正常人角质细胞中,Pelitinib对EGF诱导的EGFR磷酸化有抑制作用（IC50：20-80 nM）,还抑制STAT3的磷酸化（IC50：30-70 nM）。 Pelitinib对正常人角质细胞（IC50：61 nM）,以及A431（IC50：125 nM）和MDA-468（IC50：260 nM）肿瘤细胞的增殖有明显抑制作用,但对MCF-7细胞活性较低（IC50：3.6 μM）。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 4.68 mg/mL (10 mM), Sonication is recommended.
关键字	inhibit \| Src \| EKB569 \| HER1 \| Pelitinib \| Epidermal growth factor receptor \| Inhibitor \| WAY-EKB-569 \| ErbB-1 \| EGFR \| WAY-EKB569 \| EKB 569
相关产品	Lidocaine hydrochloride \| Lapatinib \| Neratinib \| Lidocaine \| Gefitinib \| Erlotinib \| Osimertinib \| Erlotinib hydrochloride \| Dabrafenib \| Genistein \| Regorafenib \| Sorafenib
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培利替尼|||WAY-EKB 569|||EKB-569|TargetMol

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