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531126 MPNST Inhibitor, Cpd21 - Calbiochem

531126
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₀H₈N₂OS

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      Glass bottle 25 mg
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      Description
      OverviewA cell-permeable, bioavailable, non-toxic pyridinylthiophene-carboxamide compound that preferentially and reversibly inhibits the growth of malignant peripheral nerve sheath tumors (MPNSTs) in both human and murine models in a dose-dependent manner (EC50 = 439 nM, 754 nM, and 1.0 µM in S462, SNF96.2, and sMPNST cells). Exhibits toxicity towards neurofibromatosis type 1 (Nf1) and p53 deficient MPNST cells, but does not affect normally dividing Schwann cells and mouse embryonic fibroblasts. Shown to reduce ATP consumption by all MPNST cells studied (EC50 = 1.0 µM). Synergizes with PI-3 Kinase inhibitor, LY-294002 (Cat. Nos. 440202 & 440204) to block the growth of MPNST cells. Reduces the expression of cyclin A2, B1, D1, E, cdk4, and cdk6 and increases the expression of cdkn1a and cdkn2a in a dose dependent manner. Blocks cell cycle at G1/S phase leading to apoptosis in cancer cells. Displays favorable pharmacokinetic profile and is rapidly distributed from the plasma into sMPNST tissues and has a half-life of 6-8 hours in sMPNST tissue following its complete distribution. Reduces MPNST burden in a mouse allograft model and enhances survival (~40 mg/kg, i.p. in mice for 4 weeks).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number531126
      Brand Family Calbiochem®
      SynonymsN-(Pyridin-3-yl)thiophene-2-carboxamide, Malignant Peripheral Nerve Sheath Tumors Inhibitor, Cpd 21
      References
      ReferencesChau, V., et al. 2013. Cancer Res. 74, 586.
      Product Information
      FormLight beige solid
      Hill FormulaC₁₀H₈N₂OS
      Chemical formulaC₁₀H₈N₂OS
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      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 Ambient Temperature Only
      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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      MPNST Inhibitor, Cpd21 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Chau, V., et al. 2013. Cancer Res. 74, 586.
      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.

      Revision31-July-2014
      SynonymsN-(Pyridin-3-yl)thiophene-2-carboxamide, Malignant Peripheral Nerve Sheath Tumors Inhibitor, Cpd 21
      DescriptionA cell-permeable, bioavailable, non-toxic pyridinylthiophene-carboxamide compound that preferentially and reversibly inhibits the growth of malignant peripheral nerve sheath tumors (MPNSTs) in both human and murine models in a dose-dependent manner (EC50 = 439 nM, 754 nM, and 1.0 µM in S462, SNF96.2, and sMPNST cells). Exhibits toxicity towards neurofibromatosis type 1 (Nf1) and p53 deficient MPNST cells, but does not affect normally dividing Schwann cells and mouse embryonic fibroblasts. Shown to reduce ATP consumption by all MPNST cells studied (EC50 = 1.0 µM). Synergizes with PI-3 Kinase inhibitor, LY-294002 (Cat. Nos. 440202 & 440204) to block the growth of MPNST cells. Reduces the expression of cyclin A2, B1, D1, E, cdk4, and cdk6 and increases the expression of cdkn1a and cdkn2a in a dose dependent manner. Blocks cell cycle at G1/S phase leading to apoptosis in cancer cells. Displays favorable pharmacokinetic profile and is rapidly distributed from the plasma into sMPNST tissues and has a half-life of 6-8 hours in sMPNST tissue following its complete distribution. Reduces MPNST burden in a mouse allograft model and enhances survival (~40 mg/kg, i.p. in mice for 4 weeks).
      FormLight beige solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₀H₈N₂OS
      Purity≥97% by HPLC
      SolubilityDMSO (100 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 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesChau, V., et al. 2013. Cancer Res. 74, 586.