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532814 MDM2 Inhibitor, SP-141 - CAS 1253491-42-7 - Calbiochem

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

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: SP141, SP 141

Primary Target: MDM2
532814
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Aperçu

Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
1253491-42-7C₂₂H₁₆N₂O

Products

RéférenceConditionnement Qté
5328140001 Flacon en verre 10 mg
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
CAS number1253491-42-7
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
Global Trade Item Number
Référence GTIN
5328140001 04055977281927

Documentation

MDM2 Inhibitor, SP-141 - CAS 1253491-42-7 - Calbiochem FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

Références bibliographiques

Aperçu de la référence bibliographique
Wang, W., et al. 2014. Nat. Comm. 5, 5086.

Informations techniques

Titre
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.
Fiche technique

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
CAS number1253491-42-7
Chemical formulaC₂₂H₁₆N₂O
Purity≥97% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
+2°C to +8°C
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.