SP-141

SKU: orb1306205

Description

SP-141 is a small molecule MDM2 inhibitor that induces the target's auto-ubiquitination and proteasomal degradation. It demonstrates anticancer activity in vitro and has shown efficacy in reducing tumor growth in vivo in breast cancer and pancreatic cancer xenograft models.

Research Area

Cell Biology

Key Properties

• CAS Number: 1253491-42-7
• MW: 324.38
• Purity: 99.21%
• Formula: C₂₂H₁₆N₂O
• SMILES: COc1ccc2[nH]c3c(nccc3c2c1)-c1cccc2ccccc12
• Target: MDM-2/p53,Mdm2
• Solubility: DMSO:4.4 mg/mL (13.56 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.08 mM)

Bioactivity

• In Vivo:
  Injection of nude mice with SP141 (40 mg/kg/d) inhibited growth of xenograft tumors (by 75% compared with control mice), and led to regression of orthotopic tumors.
• In Vitro:
  SP141, which bound directly to MDM2, promoting its auto-ubiquitination and degradation by the proteasome. The compound reduced levels of MDM2 in pancreatic cancer cell lines, as well as their proliferation, with 50% inhibitory concentrations <0.5 μM (0.38-0.50 μM). Increasing concentrations of SP141 induced increasing levels of apoptosis and G2-M-phase arrest of pancreatic cancer cell lines, whether or not they expressed functional P53.

Storage & Handling

• Storage: 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

breast, degradation, auto-ubiquitination, cancer, pancreatic, inhibit, MDM-2/p53, Mdm2, Inhibitor, SP 141, SP141, SP-141

Compound Identifiers

PubChem CID

59620153