产品说明书
Picropodophyllin
 |
同义名 : | 苦鬼臼脂素 ;Picropodophyllotoxin;AXL1717;NSC 36407;PPP |
| CAS号 : | 477-47-4 | |
| 货号 : | A359248 | |
| 分子式 : | C22H22O8 | |
| 纯度 : | 99%+ | |
| 分子量 : | 414.405 | |
| MDL号 : | MFCD01742647 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 50 mg/mL(120.65 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
|
||
| 描述 | IGF-1R (insulin-like growth factor-1 receptor) plays a key role in transformation, growth and survival of malignant cells, and has been considered as a general and promising target for cancer treatment. Picropodophyllin is a highly specific IGF-1R receptor with IC50 value of 1nM, even does not exhibit inhibition on phosphorylation of IR, a highly homologous receptor of IGF-1R, in cells. Picropodophyllin dose dependently blocked autophosphorylation of IGF-1R induced by IGF-1, as well as its downstream AKT and ERK on phosphorylation level in P6 cells treated with Picropodophyllin at concentration ranging in 0.5-10μM for 1h after 20 hour starvation, and cell apoptosis could be observed after treatment with 0.5μM Picropodophyllin for 6h. Growth inhibition by Picropodophyllin can be observed in a panel of tumor cells from various tumor types with IC50 values≤50nM, including FM 55, SK-MEL-28, SK-MEL-5, C8161, DFB, DFW, AA (melanoma), RD-ES (sarcoma), MCF 7 (breast carcinoma), PC3 (prostate carcinoma), HepG2 (hepatoma), P6 (embryonic mouse fibroblasts) cell lines. Administration of Picropodophyllin (20mg/kg/12h) for 8-14 days blocked growth of IGF-1R-positive tumors and caused complete regression in mice xenograft model of ES-1, BE and PC3[1]. | ||
| 作用机制 | Picropodophyllin may inhibit IGF-1R autophosphorylation at the substrate level, not ATP-competitive.[1] | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| A-549 (human lung carcinoma) neoplastic cell line | Cytotoxic assay | In vitro cytotoxicity against the A-549 (human lung carcinoma) neoplastic cell line, IC50=60 nM | 14980682 | ||
| HT-29 (human colon carcinoma) neoplastic cell line | Cytotoxic assay | In vitro cytotoxicity against the HT-29 (human colon carcinoma) neoplastic cell line, IC50=60 nM | 14980682 | ||
| P-388 neoplastic cell line | Cytotoxic assay | In vitro cytotoxicity against the P-388 (from DBA/2 mouse) neoplastic cell line, IC50=60 nM | 14980682 | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.41mL 0.48mL 0.24mL |
12.07mL 2.41mL 1.21mL |
24.13mL 4.83mL 2.41mL |
