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苦鬼臼毒素 /Picropodophyllin {[allProObj[0].p_purity_real_show]}

货号:A359248 同义名: 苦鬼臼脂素 / Picropodophyllotoxin;AXL1717

Picropodophyllin (AXL1717) 是一种选择性胰岛素样生长因子-1 受体 (IGF-1R) 抑制剂,IC50 为 1 nM。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Picropodophyllin 化学结构 CAS号:477-47-4
Picropodophyllin 化学结构
CAS号:477-47-4
Picropodophyllin 3D分子结构
CAS号:477-47-4
Picropodophyllin 化学结构 CAS号:477-47-4
Picropodophyllin 3D分子结构 CAS号:477-47-4
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Picropodophyllin 纯度/质量文件 产品仅供科研

货号:A359248 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 IGF-1R Insulin Receptor 其他靶点 纯度
BMS-536924 ++

IGF-1R, IC50: 100 nM

+++

Insulin Receptor, IC50: 73 nM

MEK,FAK 98%
GSK1904529A +++

IGF-1R, IC50: 27 nM

+++

Insulin Receptor, IC50: 25 nM

98+%
Picropodophyllin ++++

IGF-1R, IC50: 1 nM

99%+
NVP-AEW541 ++

IGF-1R, IC50: 0.15 μM

++

Insulin Receptor, IC50: 0.14 μM

FLT3 99%+
NVP-ADW742 +

IGF-1R, IC50: 0.17 μM

99%
GSK1838705A +++

IGF-1R, IC50: 2 nM

++++

Insulin Receptor, IC50: 1.6 nM

ALK 99%
BMS-754807 ++++

IGF-1R, IC50: 1.8 nM

++++

Insulin Receptor, IC50: 1.7 nM

99%+
Linsitinib +++

IGF-1R, IC50: 35 nM

++

Insulin Receptor, IC50: 75 nM

99%+
AG1024 +

IGF-1R, IC50: 7 μM

+

Insulin Receptor, IC50: 57 μM

98%
PQ401 +

IGF-1R, IC50: <1 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Picropodophyllin 生物活性

靶点
  • IGF-1R

    IGF-1R, IC50:1 nM

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]

Picropodophyllin 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

Picropodophyllin 动物研究

Dose Mice: 1.5 mg/kg[2] (daily in food), 40 mg/kg[3] (p.o.), 20 mg/kg[4] (i.p.)
Administration p.o., i.p.

Picropodophyllin 实验方案

计算器
存储液制备 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

Picropodophyllin 技术信息

CAS号477-47-4
分子式C22H22O8
分子量 414.405
别名 苦鬼臼脂素 ;Picropodophyllotoxin;AXL1717;NSC 36407;PPP
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

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
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