532814 MDM2 Inhibitor, SP-141 - Calbiochem

532814
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₂H₁₆N₂O

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable pyrido[3,4-b]indole derivative that binds directly to the hydrophobic groove of MDM2 with high affinity (Ki = 28 nM) and inhibits its activity in multiple breast cancer cell lines, independent of their p53 status. Exhibits higher binding affinity than nutlin-3 (Kd = 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.
      Catalogue Number532814
      Brand Family Calbiochem®
      SynonymsSP141, SP 141
      References
      ReferencesWang, W., et al. 2014. Nat. Comm. 5, 5086.
      Product Information
      FormYellow powder
      Hill FormulaC₂₂H₁₆N₂O
      Chemical formulaC₂₂H₁₆N₂O
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetMDM2
      Primary Target K<sub>i</sub>28 nM
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      MDM2 Inhibitor, SP-141 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

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

      Technical Info

      Title
      Characterization of Estrogen Receptor α Phosphorylation Sites in Breast Cancer Tissue Using the SNAP i.d® 2.0 System
      White Paper: Further considerations of antibody validation and usage. (EMD)
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision18-March-2015 JSW
      SynonymsSP141, SP 141
      DescriptionA cell-permeable pyrido[3,4-b]indole derivative that binds directly to the hydrophobic groove of MDM2 with high affinity (Ki = 28 nM) and inhibits its activity in multiple breast cancer cell lines, independent of their p53 status. Exhibits higher binding affinity than nutlin-3 (Kd = 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.).
      FormYellow powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₂H₁₆N₂O
      Purity≥97% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesWang, W., et al. 2014. Nat. Comm. 5, 5086.