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Protein Tyrosine Kinase
IGF-1R inhibitor
-
Apoptosis related inducer
Picropodophyllin (AXL1717)
僅限科研使用
Picropodophyllin (AXL1717)
別名: AXL1717 中文名稱：苦鬼臼毒素
Picropodophyllin (PPP, AXL1717)是一種選擇性IGF-1R抑制劑，IC50為1 nM。它對IGF-IR具有高選擇性，對IR的酪氨酸磷酸化或FGF-R、PDGF-R、EGF-R沒有抑制作用。Picropodophyllin (PPP)可誘導(dǎo)凋亡并具有抗腫瘤活性。
Picropodophyllin (AXL1717) Chemical Structure
CAS: 477-47-4
產(chǎn)品質(zhì)控
批次：
純度：
99.95%
99.95
Picropodophyllin (AXL1717)相關(guān)產(chǎn)品
| 相關(guān)靶點 | Insulin Receptor | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Linsitinib (OSI-906) NVP-AEW541 BMS-754807 AG-1024 BMS-536924 GSK1904529A NVP-ADW742 NT157 PQ 401 Phospho-IRS-1 (Ser302) Antibody [K1C11] | 點擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫 細胞周期化合物庫 血管生成相關(guān)化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Picropodophyllin (PPP, AXL1717)是一種選擇性IGF-1R抑制劑，IC50為1 nM。它對IGF-IR具有高選擇性，對IR的酪氨酸磷酸化或FGF-R、PDGF-R、EGF-R沒有抑制作用。Picropodophyllin (PPP)可誘導(dǎo)凋亡并具有抗腫瘤活性。 | ||
|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | 在完整細胞中，PPP有效抑制IGF-1刺激的IGF-1R，Akt (Ser 473)和 Erk1/2磷酸化。在培養(yǎng)的IGF-1R 陽性腫瘤細胞中，Picropodophyllin特異性抑制細胞生長，并誘導(dǎo)細胞凋亡。 Picropodophyllin通過進一步降低細胞活性并增強細胞凋亡，協(xié)同使HMCL，原代人MM 和小鼠5T33MM細胞對ABT-737 和 ABT-199更敏感。 Picropodophyllin 協(xié)同抑制肝細胞癌的增殖和活性。 |
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|---|---|---|---|---|
| 激酶實驗 | 體外酪氨酸激酶試驗。 | |||
| IGF-1R催化的pTG底物磷酸化測定使用96孔板酪氨酸激酶試劑盒進行。我們使用重組表皮生長因子受體，HEPG2免疫沉淀物IR，P6細胞免疫沉淀物IGF-1R，以及來自P6 (代表“非-IGF-1R 酪氨酸激酶”)的IGF-1R免疫沉淀上清液。用所需化合物將受體在激酶緩沖液[50 mM HEPES 緩沖液(pH 7.4)，20 mM MgCl2，0.1 MnCl2，和0.2 Na3VO4]中處理30分鐘，激酶反應(yīng)通過加入ATP激活。磷酸化聚合體底物用與辣根過氧化物酶共軛的磷酸酪氨酸特異性單克隆抗體，克隆PT-66探測。通過辣根過氧化物酶底物鄰苯二胺二鹽酸化物顯色，并通過分光光度法(ELISA 閱讀器)定量。IGF-1R酪氨酸自磷酸化通過夾心ELISA法進行分析。簡而言之，96孔板用1微克/孔的IGF-1R β亞型抗體涂覆，在4℃下培養(yǎng)過夜。板用1% BSA在PBS Tween中封存1小時，然后將來自P6細胞系的總蛋白裂解物以80微克/孔加入。使用來自R細胞系的總蛋白裂解物作為陰性對照。將研究的化合物加入不含ATP的酪氨酸激酶緩沖液，在室溫下進行30分鐘，再用ATP活化激酶。激酶測定使用Sigma 試劑盒(如上)進行。分光光度法后，使用軟件程序的REGRESSION函數(shù)測定抑制劑的IC50值。 | ||||
| 細胞實驗 | 細胞系 | 黑色素瘤細胞(FM 55，SK-MEL-28，SK-MEL-5，C8161，DFB，DFW 和 AA)，肉瘤細胞(RD-ES)，乳腺癌細胞(MCF 7)，前列腺癌細胞(PC3)，肝癌細胞(HepG2)和胚胎小鼠成纖維細胞(P6 和 R-) | ||
| 濃度 | ~15 μM | |||
| 孵育時間 | 48小時 | |||
| 方法 | 測定使用細胞增殖試劑盒II，基于黃色四唑鎓鹽2,3-雙[2-甲氧基-4-硝基-5-磺苯基] -2H-四唑鎓-5-羧酰苯胺內(nèi)鹽在橙色甲瓚染料中被活細胞呼吸鏈改變色度的原理進行。所有參照標準和實驗以一式三份進行。 |
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| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | p-IGFR1 / p-AKT / p-ERK |
|
22363814 | |
| Growth inhibition assay | Cell viability |
|
22159423 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 在異種移植人ES-1，BE，和PC3的SCID小鼠體內(nèi)，Picropodophyllin (20 mg/kg/12 h, i.p.)引起完全的腫瘤退化。在5T33MM小鼠模型中，Picropodophyllin也表現(xiàn)出有效的抗腫瘤活性，并使存活率顯著增加。 |
|
|---|---|---|
| 動物實驗 | Animal Models | 負荷表達IGF-1R，或 R- v-src (IGF-1R 陰性) 和 P12 (過表達 IGF-1 和 IGF-1R)的 ES-1，BE，或 PC3 異種移植物的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 G?genur|Nyk?bing Falster County Hospital|Naestved Hospital|Holbaek Sygehus|Slagelse Hospital|Zealand University Hospital |
October 1 2022 | Not Applicable |
|
化學(xué)信息&溶解度
| 分子量 | 414.41 | 分子式 | C22H22O8 |
| CAS號 | 477-47-4 | SDF | Download Picropodophyllin (AXL1717) SDF |
| Smiles | COC1=CC(=CC(=C1OC)OC)C2C3C(COC3=O)C(C4=CC5=C(C=C24)OCO5)O | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 83 mg/mL ( (200.28 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 1.5 mg/mL (3.61 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | |||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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* 必填項
常見問題及建議解決方法
問題 1:
I am currently setting the conditions for in vivo experiments, how should I reconstitute it?
回答：
Other than DMSO:vegetable oil 10:1 (v/v) cited from reference. We tested another formulation: 4% DMSO+corn oil. This compound 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.
