Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Picropodophyllin (Picropodophyllin (PPP)) 是一种选择性的胰岛素样生长因子-1受体抑制剂,IC50为1 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 225 | 现货 | ||
5 mg | ¥ 498 | 现货 | ||
10 mg | ¥ 692 | 现货 | ||
25 mg | ¥ 1,450 | 现货 | ||
50 mg | ¥ 2,660 | 现货 | ||
100 mg | ¥ 4,000 | 现货 | ||
500 mg | ¥ 8,750 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 545 | 现货 |
产品描述 | 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). |
靶点活性 | IGF-1R:1 nM |
体外活性 | In intact cells, PPP efficiently inhibits IGF-1-stimulated IGF-1R, Akt (Ser 473) and Erk1/2 phosphorylation. Picropodophyllin specifically inhibits cell growth, and induces apoptosis in cultured IGF-1R-positive tumor cells. [1] Picropodophyllin synergistically sensitizes HMCL, primary human MM and murine 5T33 mM cells to ABT-737 and ABT-199 by further decreasing cell viability and enhancing apoptosis. [3] Picropodophyllin and sorafenib synergistically suppress the proliferation and motility of hepatocellular carcinoma cells. [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] |
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. |
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) |
别名 | AXL1717, 苦鬼臼脂素, Picropodophyllin (PPP), Picropodophyllotoxin, PPP, 苦鬼臼毒素 |
分子量 | 414.41 |
分子式 | C22H22O8 |
CAS No. | 477-47-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 76 mg/mL (183.4 mM)
Ethanol: 1 mg/mL (2.41 mM), Heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.4131 mL | 12.0653 mL | 24.1307 mL | 60.3267 mL |
DMSO | 5 mM | 0.4826 mL | 2.4131 mL | 4.8261 mL | 12.0653 mL |
10 mM | 0.2413 mL | 1.2065 mL | 2.4131 mL | 6.0327 mL | |
20 mM | 0.1207 mL | 0.6033 mL | 1.2065 mL | 3.0163 mL | |
50 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2065 mL | |
100 mM | 0.0241 mL | 0.1207 mL | 0.2413 mL | 0.6033 mL |
中药材名称 | 中药材拉丁名 | 性 | 味 | 归经 |
三颗针 | Berberis soulieana Schneid., Berberis wilsonae Hems, Berberis poiretii Schneid., Berberis vernae Schneid. | 寒 | 苦 | 肝, 胃, 大肠 |
中成药名称 | 处方组成 | 主治疾病 | 中成药类型 |
宁泌泰胶囊 | 四季红,芙蓉叶,仙鹤草,大风藤,白茅根,连翘,三颗针 | 口服,一次3~4粒,一日3次;7天为一个疗程,或遵医嘱。 | 祛湿药 |
双黄消炎片 | 三颗针,黄芩 | 口服,一次 3片,一日 3次。 | 清热药 |
降糖胶囊 | 人参,知母,三颗针,干姜,五味子,人参茎叶皂甙 | 口服,一次4~6粒,一日3次。 | 补益药 |
双黄消炎胶囊 | 三颗针,黄芩 | 口服。一次3粒,一日3次。 | 扶正药 |
清热治痢丸 | 马齿苋,三颗针 | 口服,一次6g,一日 3次。 | 清热药 |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Picropodophyllin 477-47-4 Apoptosis Tyrosine Kinase/Adaptors IGF-1R Inhibitor AXL1717 苦鬼臼脂素 Picropodophyllin (PPP) Picropodophyllotoxin AXL-1717 PPP inhibit 苦鬼臼毒素 AXL 1717 inhibitor