5.32814

MDM2 Inhibitor, SP-141

• Synonyma: MDM2 Inhibitor, SP-141, SP141, SP 141
• Empirický vzorec (Hillův zápis): C₂₂H₁₆N₂O
• Číslo CAS: 1253491-42-7
• Molekulová hmotnost: 324.38
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD29059920
• Assay: ≥97% (HPLC)
• Form: powder
• Storage condition: OK to freeze, protect from light

Vlastnosti

• assay: ≥97% (HPLC)
• Quality Segment: 100
• form: powder
• potency: 28 nM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: yellow
• solubility: DMSO: 50 mg/mL
• storage temp.: 2-8°C
• SMILES string: COC1=CC=C(NC2=C3C=CN=C2C4=CC=CC5=C4C=CC=C5)C3=C1
• InChI: 1S/C22H16N2O/c1-25-15-9-10-20-19(13-15)18-11-12-23-21(22(18)24-20)17-8-4-6-14-5-2-3-7-16(14)17/h2-13,24H,1H3
• InChI key: AABFWJDLCCDJJN-UHFFFAOYSA-N

Popis

General description

A cell-permeable compound that binds to MDM2 with high affinity (K_i = 28 nM) and inhibits its activity in multiple breast cancer cell lines, independent of their p53 status.

A cell-permeable pyrido[3,4-b]indole derivative that binds directly to the hydrophobic groove of MDM2 with high affinity (K_i = 28 nM) and inhibits its activity in multiple breast cancer cell lines, independent of their p53 status. Exhibits higher binding affinity than nutlin-3 (K_d = 45 nM). Acts by reducing MDM2 expression and promoting its ubiquitination and proteasomal degradation. Induces cell cycle arrest at the G2 phase and induces apoptosis in MCF-7, MCF-7 KD, and MDA-MB-468 breast cancer cells in a concentration-dependent manner. Also reported to diminish cell migration and reduce metastasis of breast cancer cells. Suppresses the growth of MCF-7 and MDA-MB-468 xenografts in nude mice (40 mg/kg/ 30 or 42 days, i.p.).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
MDM2

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Wang, W., et al. 2014. Nat. Comm.5, 5086.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Bezpečnostní informace

• Skladovací třída: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable