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AXL1717 (picropodophyllin, Picropodophyllotoxin, PPP) is a non-competitive, potent, and specific inhibitor of IGF-1Rα/β with IC50 of 1 nM. It exhibits little effect towards IR, FGFR, PDGFR and EGFR, and exerts no effects on microtubules and DNA topoisomerase II. Picropodophyllotoxin inhibits IGF1R autophosphorylation (IC50 ~ 1 nM), increases the fraction of cells in the G2/M phase and upregulates apoptosis.It also exhibits antiproliferative effects in multiple cancer cell lines (IC50 = 0.05 - 15 μM). In vivo,it has anticancer and antineovascularization activity.
Another CAS# 17434-18-3
J Invest Dermatol. 2024 Sep 16.
Deciphering the Dysregulating IGF-1-SP1-CD248 Pathway in Fibroblast Functionality during Diabetic Wound Healing
Picropodophyllin (AXL1717) purchased from AbMole
Neuroreport. 2019 May 22;30(8):580-585.
Insulin attenuates epileptiform discharge-induced oxidative stress by increasing zinc-α2-glycoprotein in primary cultured cortical neurons.
Picropodophyllin (AXL1717) purchased from AbMole
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Source | Cancer Sci (2018). Figure 4. AXL1717 |
| Method | MTT assay | |
| Cell Lines | MKN7 cells | |
| Concentrations | 500 nmol/L | |
| Incubation Time | 3 days | |
| Results | The cell proliferation ratios of the cells treated with afatinib, neratinib, or PPP compared with a control were 62.3%, 45.9%, and 54.1%, respectively. |
| Cell Experiment | |
|---|---|
| Cell lines | HUVEC cells |
| Preparation method | The HUVEC cells were trypsinized, harvested and plated onto 96-well flat-bottom plates at a density of 1,000 cells per well. Following 24 h of culture, sorafenib or PPP was added to the medium. After 72 h of incubation, a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium inner salt (MTS) assay was performed following the manufacturer’s instructions. |
| Concentrations | 0.2 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | ALB/c nude mice |
| Formulation | DMSO |
| Dosages | 20 mg/kg |
| Administration | Intraperitoneal injection |
| Molecular Weight | 414.41 |
| Formula | C22H22O8 |
| CAS Number | 477-47-4 |
| Solubility (25°C) | DMSO ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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