苦鬼臼毒素|T6943|TargetMol

Picropodophyllin
477-47-4

￥225 1mg 起订

￥498 5mg 起订

￥692 10mg 起订

上海更新日期：2024-12-02

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产品详情:

中文名称：: 苦鬼臼毒素

英文名称：: Picropodophyllin

CAS号：: 477-47-4

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：: 99.55%

产品类别：: 抑制剂

货号：: T6943

Product Introduction

Bioactivity

名称	Picropodophyllin
描述	Picropodophyllin (Picropodophyllin (PPP)) (PPP) is a specific IGF-1R inhibitor (IC50: 1 nM). Picropodophyllin specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast/stem cell growth factor (KIT).
细胞实验	The determinations are performed using the Cell proliferation kit II, which is based on colorimetric change of the yellow tetrazolium salt 2,3-bis[2-methoxy-4-nitro-5-sulfophenyl]-2H-tetrazolium-5-carboxanilide inner salt in orange formazan dye by the respiratory chain of viable cell. All of the standards and experiments are performed in triplicates. (Only for Reference)
激酶实验	In vitro tyrosine kinase assays.: Assay of IGF-1R-catalyzed substrate phosphorylation of pTG, using a 96-well plate tyrosine kinase assay kit, is performed. We use recombinant epidermal growth factor receptor, immunoprecipitated IR from HEPG2, immunoprecipitated IGF-1R from P6 cells, and IGF-1R immunodepleted supernatant from P6 (representing "non-IGF-1R tyrosine kinases"). After 30-min treatment of the receptors with the desired compounds in the kinase buffer [50 mM HEPES buffer (pH 7.4), 20 mM MgCl2, 0.1 MnCl2, and 0.2 Na3VO4], the kinase reaction is activated by addition of ATP. The phosphorylated polymer substrate is probed with a phosphotyrosine-specific monoclonal antibody conjugated to horseradish peroxidase, clone PT-66. Color is developed with horseradish peroxidase chromogenic substrate O-phenylenediamine dihydrochloride and quantitated by spectrophotometry (ELISA reader). IGF-1R tyrosine autophosphorylation is analyzed by a sandwich ELISA assay. Briefly, 96-well plates are coated overnight at 4°C with 1 μg/well of an antibody to IGF-1R β-subunit. The plates are blocked with 1% BSA in PBS Tween for 1 h, and then 80 μg/well of total protein lysate from the P6 cell line is added. As a negative control we use total protein lysate from the R- cell line. The investigated compounds are added in tyrosine kinase buffer without ATP at room temperature for 30 min before kinase activation with ATP. Kinase assay is performed using the Sigma kit (see above). After spectrophotometry the IC50 values of inhibitors are determined using the REGRESSION function of Statistica program.
体外活性	在完整细胞中，PPP有效抑制IGF-1激活的IGF-1R、Akt (Ser 473)和Erk1/2的磷酸化。Picropodophyllin特异性抑制细胞生长，并在培养的IGF-1R阳性肿瘤细胞中诱导凋亡。[1] Picropodophyllin与ABT-737和ABT-199协同作用，通过进一步降低细胞活性和增强凋亡，从而增强对HMCL、原发性人MM细胞和小鼠5T33 mM细胞的敏感性。[3] Picropodophyllin和索拉非尼协同抑制肝细胞癌细胞的增殖和移动性。[4]
体内活性	在SCID小鼠中，通过人类ES-1、BE和PC3细胞外植后，Picropodophyllin（20 mg/kg/12 h，i.p.）能引起肿瘤完全消退。[1] 在5T33 mM小鼠模型中，Picropodophyllin同样展现出显著的抗肿瘤活性，并显著延长生存期。[2]
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) DMSO : 55 mg/mL (132.72 mM), Sonication is recommended. Ethanol : 1 mg/mL (2.41 mM), Heating is recommended.
关键字	Inhibitor \| IGF-1R \| Apoptosis \| AXL-1717 \| inhibit \| Picropodophyllin \| AXL 1717
相关产品	L-Glutamic acid \| Metronidazole \| 5-Fluorouracil \| Dextran sulfate sodium salt (MW 4500-5500) \| Stavudine \| Tributyrin \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Acetylcysteine \| Salicylic acid \| Sodium 4-phenylbutyrate
相关库	抑制剂库 \| 抗癌活性化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 高选择性抑制剂库 \| 天然产物库 \| 酪氨酸激酶分子库 \| 高通量筛选天然产物库 \| 抗癌药物库

苦鬼臼脂素|||苦鬼臼毒素|||PPP|||Picropodophyllotoxin|||Picropodophyllin (PPP)|||AXL1717|TargetMol

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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