Picropodophyllin (PPP)
别名: AXL1717 中文名称：苦鬼臼毒素
Picropodophyllin (PPP, AXL1717)是一种选择性IGF-1R抑制剂，IC50为1 nM。它对IGF-IR具有高选择性，对IR的酪氨酸磷酸化或FGF-R、PDGF-R、EGF-R没有抑制作用。Picropodophyllin (PPP)可诱导凋亡并具有抗肿瘤活性。
Picropodophyllin (PPP) Chemical Structure
CAS: 477-47-4
产品质控
批次：
纯度：
99.95%
99.95
Picropodophyllin (PPP)相关产品
| 相关靶点 | Insulin Receptor | 点击展开 |
|---|---|---|
| 相关产品 | Linsitinib (OSI-906) NVP-AEW541 BMS-754807 GSK1904529A BMS-536924 AG-1024 NVP-ADW742 NT157 PQ 401 | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 酪氨酸激酶抑制剂分子库 PI3K/Akt 抑制剂库 细胞周期化合物库 血管生成相关化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 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 | ||
| amnion cells | Antiviral assay | Antiviral activity against HSV1 infected in human primary amnion cells assessed as inhibition of virus-induced pathogenic effect, Activity = 1.9 μM. | 9834179 | ||
| P388 | Cytotoxicity assay | Cytotoxicity against mouse P388 cells, IC50 = 6 μM. | 7673931 | ||
| A549 | Cytotoxicity assay | Cytotoxicity against human A549 cells, IC50 = 6 μM. | 7673931 | ||
| HT-29 | Cytotoxicity assay | Cytotoxicity against human HT-29 cells, IC50 = 6 μM. | 7673931 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Picropodophyllin (PPP, AXL1717)是一种选择性IGF-1R抑制剂，IC50为1 nM。它对IGF-IR具有高选择性，对IR的酪氨酸磷酸化或FGF-R、PDGF-R、EGF-R没有抑制作用。Picropodophyllin (PPP)可诱导凋亡并具有抗肿瘤活性。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在完整细胞中，PPP有效抑制IGF-1刺激的IGF-1R，Akt (Ser 473)和 Erk1/2磷酸化。在培养的IGF-1R 阳性肿瘤细胞中，Picropodophyllin特异性抑制细胞生长，并诱导细胞凋亡。[1] Picropodophyllin通过进一步降低细胞活性并增强细胞凋亡，协同使HMCL，原代人MM 和小鼠5T33MM细胞对ABT-737 和 ABT-199更敏感。[3] Picropodophyllin 协同抑制肝细胞癌的增殖和活性。[4] |
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|---|---|---|---|---|
| 激酶实验 | 体外酪氨酸激酶试验。 | |||
| IGF-1R催化的pTG底物磷酸化测定使用96孔板酪氨酸激酶试剂盒进行。我们使用重组表皮生长因子受体，HEPG2免疫沉淀物IR，P6细胞免疫沉淀物IGF-1R，以及来自P6 (代表“非-IGF-1R 酪氨酸激酶”)的IGF-1R免疫沉淀上清液。用所需化合物将受体在激酶缓冲液[50 mM HEPES 缓冲液(pH 7.4)，20 mM MgCl2，0.1 MnCl2，和0.2 Na3VO4]中处理30分钟，激酶反应通过加入ATP激活。磷酸化聚合体底物用与辣根过氧化物酶共轭的磷酸酪氨酸特异性单克隆抗体，克隆PT-66探测。通过辣根过氧化物酶底物邻苯二胺二盐酸化物显色，并通过分光光度法(ELISA 阅读器)定量。IGF-1R酪氨酸自磷酸化通过夹心ELISA法进行分析。简而言之，96孔板用1微克/孔的IGF-1R β亚型抗体涂覆，在4℃下培养过夜。板用1% BSA在PBS Tween中封存1小时，然后将来自P6细胞系的总蛋白裂解物以80微克/孔加入。使用来自R细胞系的总蛋白裂解物作为阴性对照。将研究的化合物加入不含ATP的酪氨酸激酶缓冲液，在室温下进行30分钟，再用ATP活化激酶。激酶测定使用Sigma 试剂盒(如上)进行。分光光度法后，使用软件程序的REGRESSION函数测定抑制剂的IC50值。 | ||||
| 细胞实验 | 细胞系 | 黑色素瘤细胞(FM 55，SK-MEL-28，SK-MEL-5，C8161，DFB，DFW 和 AA)，肉瘤细胞(RD-ES)，乳腺癌细胞(MCF 7)，前列腺癌细胞(PC3)，肝癌细胞(HepG2)和胚胎小鼠成纤维细胞(P6 和 R-) | ||
| 浓度 | ~15 μM | |||
| 孵育时间 | 48小时 | |||
| 方法 | 测定使用细胞增殖试剂盒II，基于黄色四唑鎓盐2,3-双[2-甲氧基-4-硝基-5-磺苯基] -2H-四唑鎓-5-羧酰苯胺内盐在橙色甲瓒染料中被活细胞呼吸链改变色度的原理进行。所有参照标准和实验以一式三份进行。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-IGFR1 / p-AKT / p-ERK |
|
22363814 | |
| Growth inhibition assay | Cell viability |
|
22159423 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在异种移植人ES-1，BE，和PC3的SCID小鼠体内，Picropodophyllin (20 mg/kg/12 h, i.p.)引起完全的肿瘤退化。[1]在5T33MM小鼠模型中，Picropodophyllin也表现出有效的抗肿瘤活性，并使存活率显著增加。[2] |
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|---|---|---|
| 动物实验 | Animal Models | 负荷表达IGF-1R，或 R- v-src (IGF-1R 阴性) 和 P12 (过表达 IGF-1 和 IGF-1R)的 ES-1，BE，或 PC3 异种移植物的SCID小鼠 |
| Dosages | 20 mg/kg/12 h | |
| Administration | i.p. | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06357884 | Recruiting | Diabetic Neuropathies|Plantar Callus |
Chinese University of Hong Kong|Princess Margaret Hospital Hong Kong |
February 23 2024 | Not Applicable |
| NCT05710185 | Recruiting | Palmoplantar Pustulosis |
Brigham and Women''s Hospital|University of Pennsylvania |
July 1 2023 | Phase 4 |
| NCT06025422 | Recruiting | Diabetic Foot Ulcer|Diabetic Neuropathies |
University Hospitals Leicester|University of Salford |
March 13 2023 | -- |
| NCT04433052 | Recruiting | Coronary Heart Disease |
Tampere University |
February 1 2023 | Not Applicable |
| NCT05740137 | Active not recruiting | Colorectal Cancer|Colorectal Adenoma|Colorectal Neoplasms |
Ismail Gögenur|Nykøbing Falster County Hospital|Naestved Hospital|Holbaek Sygehus|Slagelse Hospital|Zealand University Hospital |
October 1 2022 | Not Applicable |
化学信息&溶解度
| 分子量 | 414.41 | 分子式 | C22H22O8 |
| CAS号 | 477-47-4 | SDF | Download Picropodophyllin (PPP) SDF |
| Smiles | COC1=CC(=CC(=C1OC)OC)C2C3C(COC3=O)C(C4=CC5=C(C=C24)OCO5)O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 83 mg/mL ( (200.28 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 1.5 mg/mL (3.61 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
I am currently setting the conditions for in vivo experiments, how should I reconstitute the drug?
回答：
Other than DMSO:vegetable oil 10:1 (v/v) cited from reference. We tested another formulation: 4% DMSO+corn oil. S7668 Picropodophyllin (PPP) can be dissolved in it at 5 mg/ml clearly. But after stayed for about 20-30 min, the two phase would separate and wouldn't get together again. So if you are going to use this formulation, please prepare the fresh solution just before use.
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