5.32814

MDM2 Inhibitor, SP-141

• Sinônimo(s): MDM2 Inhibitor, SP-141, SP141, SP 141
• Fórmula empírica (Notação de Hill): C₂₂H₁₆N₂O
• Número CAS: 1253491-42-7
• Peso molecular: 324.38
• Número MDL: MFCD29059920
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥97% (HPLC)
• Nível de qualidade: 100
• forma: powder
• potência: 28 nM K_i
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: yellow
• solubilidade: DMSO: 50 mg/mL
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres SMILES: COC1=CC=C(NC2=C3C=CN=C2C4=CC=CC5=C4C=CC=C5)C3=C1

Descrição

Descrição geral

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.).

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.).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
MDM2

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable