5.32814

MDM2 Inhibitor, SP-141

• 別名: MDM2 Inhibitor, SP-141, SP141, SP 141
• 実験式（ヒル表記法）: C₂₂H₁₆N₂O
• CAS番号: 1253491-42-7
• 分子量: 324.38
• MDL番号: MFCD29059920
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥97% (HPLC)
• 品質水準: 100
• 形状: powder
• 有効性: 28 nM K_i
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: yellow
• 溶解性: DMSO: 50 mg/mL
• 保管温度: 2-8°C
• SMILES記法: COC1=CC=C(NC2=C3C=CN=C2C4=CC=CC5=C4C=CC=C5)C3=C1

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
MDM2

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable