SP 141

SKU: orb1220032

Description

SP 141 is a MDM2 inhibitor.SP-141 promotes MDM2 auto-ubiquitination and degradation, with anticancer activity.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. 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.

Key Properties

• CAS Number: 1253491-42-7
• MW: 324.38
• Purity: >98% (HPLC)
• Formula: C₂₂H₁₆N₂O
• SMILES: COc1ccc2[nH]c3c(nccc3c2c1)-c1cccc2ccccc12
• Target: MDM2-p53
• Solubility: In Vitro: DMSO : 125 mg/mL (385.35 mM)

Bioactivity

• In Vivo:
  Animal model: Nude mice bearing Panc-1 xenograft tumors. Dosage: 40 mg/kg. Administration: Administered by i.p. injection; 5 d/wk for about three weeks. Result: Significantly suppressed the growth of pancreatic xenograft tumors. On Day 18, the tumor volume in the treated group was reduced by 75% compared with that in the control group. There were no significant differences in the body weight compared with the control group.
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• In Vitro:
  Cell Viability Assay Cell line: HPAC, Panc-1, AsPC-1, and Mia-Paca-2 pancreatic cancer cell lines. Human primary fibroblasts (IMR90) Concentration: 0.01, 0.1, 1, and 10 μM Incubation time: 72 hours. Result: IC50s of 0.38, 0.50, 0.36, 0.41, and 13.22 μM for HPAC, Panc-1, AsPC-1, Mia-Paca-2, and IMR90, respectively. Western blot analysis. Cell line: HPAC and Panc-1 cells. Concentration: 0.5 μM Incubation time: 120 minutes. Result: Reduced the MDM2 protein levels. Increased the degradation rate of the MDM2 protein in the presence of Cycloheximide (15 μg/mL).
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

MDM2-p53