Picropodophyllin

SKU: orb1300325

Description

Picropodophyllin (PPP) is a potent and selective IGF-1R inhibitor with an IC50 of 1 nM. It downregulates IGF1R expression without affecting related receptors like InsR. This specificity makes it a valuable research tool for studying IGF-1R signaling in cancer models, both in vitro and in vivo.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 477-47-4
• MW: 414.41
• Purity: 99.83%
• Formula: C₂₂H₂₂O₈
• SMILES: [H][C@]12COC(=O)[C@@]1([H])[C@H](c1cc(OC)c(OC)c(OC)c1)c1cc3OCOc3cc1[C@@H]2O
• Target: Apoptosis,IGF-1R
• Solubility: Ethanol:1 mg/mL (2.41 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.83 mM);DMSO:61.25 mg/mL (147.8 mM)

Bioactivity

• Target IC50:
  IGF-1R:1 nM
• In Vivo:
  In SCID mice xenografted with human ES-1, BE, and PC3, Picropodophyllin (20 mg/kg/12 h, i.p.) causes complete tumor regression. In the 5T33 mM mouse model, Picropodophyllin also shows a marked antitumor activity, and causes a significant increase in survival.
• In Vitro:
  In intact cells, PPP efficiently inhibits IGF-1-stimulated IGF-1R, Akt (Ser 473) and Erk1/2 phosphorylation. Picropodophyllin specifically inhibits cell growth, and induces apoptosis in cultured IGF-1R-positive tumor cells. Picropodophyllin synergistically sensitizes HMCL, primary human MM and murine 5T33 mM cells to ABT-737 and ABT-199 by further decreasing cell viability and enhancing apoptosis. Picropodophyllin and sorafenib synergistically suppress the proliferation and motility of hepatocellular carcinoma cells.
• Cell Research:
  The determinations are performed using the Cell proliferation kit II, which is based on colorimetric change of the yellow tetrazolium salt 2,3-bis[2-methoxy-4-nitro-5-sulfophenyl]-2H-tetrazolium-5-carboxanilide inner salt in orange formazan dye by the respiratory chain of viable cell. All of the standards and experiments are performed in triplicates. (Only for Reference)

Storage & Handling

• Storage: keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AXL 1717, AXL1717, AXL-1717, Apoptosis, IGF-1R, IGF1R, Picropodophyllin, Picropodophyllin (PPP), Picropodophyllotoxin, PPP

Compound Identifiers

PubChem CID

72435