1253491-42-7
1253491-42-7 structure
- Name: SP 141
- Chemical Name: sp-141
- CAS Number: 1253491-42-7
- Molecular Formula: C22H16N2O
- Molecular Weight: 324.37500
- Catalog: Signaling Pathways Apoptosis MDM-2/p53
- Create Date: 2018-01-02 16:33:59
- Modify Date: 2024-01-10 18:17:57
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SP-141 is a specific inhibitor of MDM2. SP-141 promotes MDM2 auto-ubiquitination and degradation. SP-141 might be used for the research of pancreatic cancer and breast cancer cells[1].
| Name | sp-141 |
|---|---|
| Synonyms |
6-methoxy-1-naphthalen-1-yl-9H-β-carboline
6-methoxy-1-(naphthalen-1-yl)-9H-pyrido[3,4-b]indole |
| Description | SP-141 is a specific inhibitor of MDM2. SP-141 promotes MDM2 auto-ubiquitination and degradation. SP-141 might be used for the research of pancreatic cancer and breast cancer cells[1]. |
|---|---|
| Related Catalog | |
| Target |
MDM2[1] |
| In Vitro | SP-141 (0.01-10 μM; 72 hours) inhibits human pancreatic cancer cell growth with IC50 values of less than 0.5 μM (0.38-0.50 μM) in a p53-independent manner. The IMR90 cells are much less sensitive to SP141 than the pancreatic cancer cells, suggesting that SP141 has a selective cytotoxicity for cancer cells[1]. SP141 induces MDM2 auto-ubiquitination and proteasomal degradation in both HPAC and Panc-1 cells[1]. Cell Viability Assay[1] 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[1] 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). |
| In Vivo | SP-141 (40 mg/kg; administered by i.p. injection; 5 d/wk for about three weeks) suppresses pancreatic tumor growth in both xenograft and orthotopic mouse models[1]. Animal Model: Nude mice bearing Panc-1 xenograft tumors[1] 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. |
| References |
| Molecular Formula | C22H16N2O |
|---|---|
| Molecular Weight | 324.37500 |
| Exact Mass | 324.12600 |
| PSA | 37.91000 |
| LogP | 5.54490 |