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
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. |
| 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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related IGF-1R Products |
|---|
| IGF-I (24-41)
IGF-I (24-41) (Insulin-like Growth Factor I (24-41)) is amino acids 24 to 41 fragment of IGF-I. |
| GIP, human
GIP, human is a peptide hormone consisting of 42 amino acids that also acts as a promoter of glucose-dependent insulin secretion and a weak inhibitor of gastric acid secretion. In addition, GIP, human acts as an enteric proinsulin hormone released by intestinal K cells in response to nutrient intake. |
| VMB-100
VMB-100 is an engineered mRNA molecule encoding human insulin-like growth factor-1 (IGF-1) that induces IGF-1 expression in human muscle cells. |
| NBI-31772 hydrate
NBI-31772 hydrate is a potent inhibitor of interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). NBI-31772 hydrate is also a nonpeptide ligand that releases bioactive IGF-I from the IGF-I/IGFBP-3 complex (Kis=1-24 nM for all six human subtypes). Anxiolytic and antidepressant-like effects. |
| AZ12253801
AZ12253801 is an ATP-competitive IGF-1R tyrosine kinase inhibitor that shows ∼10-fold selectivity over the insulin receptor. AZ12253801 inhibits IGF-1R–driven proliferation in 3T3 mouse fibroblasts (transfected with human IGF-1R) with an IC50 of 17 nmol/L. The IC50 for epidermal growth factor receptor (EGFR)–driven proliferation is 440 nmol/L. Anti-tumor activity. |
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