573110 STAT5 Inhibitor III, Pimozide - CAS 2062-78-4 - Calbiochem

573110
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₈H₂₉F₂N₃O 2062-78-4

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      573110-100MG
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          Glass bottle 100 mg
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          Description
          OverviewA cell-permeable and orally available diphenylbutylpiperidine class of psychotropic drug with antagonistic activity against DAT (dopamine transporter) as well as several postsynaptic receptors, including D1, D2, D3, D4, α1-/α2-adrenergic, and 5-HT2A receptors. In addition to its antipsychotic property, Pimozide is shown to inhibit the constitutive STAT5 Tyr694 phosphorylation (5 to 10 µM for 3h) and transcription activity (5 µM for 18 h) in Bcr-Abl+ K562 and KU812 cultures, while exhibiting little activity against IFNα-stimulated STAT1 phosphorylation or LIF-stimulated STAT3 phosphorylation in K562 cells (10 µM 1 h pretreatment). The mechanism of STAT5 inhibition is currently unknown and Primozide is reported to exhibit little inhibitory activity against cellular Bcr-Abl autophosphorylation or the kinase activities of Abl1 (Wt & T315I), Hck, Lyn A/B, and Src (≤7%) in cell-free kinase assays. Shown to exhibit selective antiproliferative activity against K562, KU812, and primary bone marrow mononuclear cells from CML patients (by >80%; 10 µM for 48 h), but not peripheral blood mononuclear cells from healthy individuals, due to G0/G1 cell cycle arrest and apoptosis induction.
          Catalogue Number573110
          Brand Family Calbiochem®
          Synonyms1-(1-(4,4-Bis(4-fluorophenyl)butyl)-4-piperidinyl)-1,3-dihydro-2H-benzimidazol-2-one
          References
          ReferencesChen, J., et al. 2011. Chem. Biol 18, 1390.
          Nelson, E.A., et al. 2011. Blood 117, 3421.
          Product Information
          CAS number2062-78-4
          FormWhite solid
          Hill FormulaC₂₈H₂₉F₂N₃O
          Chemical formulaC₂₈H₂₉F₂N₃O
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥98% by HPLC
          Physicochemical Information
          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 Regulatory Review
          Storage -20°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions ar 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

          STAT5 Inhibitor III, Pimozide - CAS 2062-78-4 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          STAT5 Inhibitor III, Pimozide - CAS 2062-78-4 - Calbiochem Certificates of Analysis

          TitleLot Number
          573110

          References

          Reference overview
          Chen, J., et al. 2011. Chem. Biol 18, 1390.
          Nelson, E.A., et al. 2011. Blood 117, 3421.
          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.

          Revision28-November-2011 JSW
          Synonyms1-(1-(4,4-Bis(4-fluorophenyl)butyl)-4-piperidinyl)-1,3-dihydro-2H-benzimidazol-2-one
          DescriptionA cell-permeable and orally available diphenylbutylpiperidine class of psychotropic drug with antagonistic activity against DAT (dopamine transporter) as well as several postsynaptic receptors, including D1, D2, D3, D4, α1-/α2-adrenergic, and 5-HT2A receptors. In addition to its antipsychotic property, Pimozide is shown to inhibit the constitutive STAT5 Tyr694 phosphorylation (5 to 10 µM for 3h) and transcription activity (5 µM for 18 h) in Bcr-Abl+ K562 and KU812 cultures, while exhibiting little activity against IFNα-stimulated STAT1 phosphorylation or LIF-stimulated STAT3 phosphorylation in K562 cells (10 µM 1 h pretreatment). The mechanism of STAT5 inhibition is currently unknown and Primozide is reported to exhibit little inhibitory activity against cellular Bcr-Abl autophosphorylation or the kinase activities of Abl1 (Wt & T315I), Hck, Lyn A/B, and Src (≤7%) in cell-free kinase assays. Shown to exhibit selective antiproliferative activity against K562, KU812, and primary bone marrow mononuclear cells from CML patients (by >80%; 10 µM for 48 h), but not peripheral blood mononuclear cells from healthy individuals, due to G0/G1 cell cycle arrest and apoptosis induction. Acts as a selective and non-competitive inhibitor of human USP1/UAF1 and USP7 activities (IC50 = 2 and 47 µM, respectively) with no effect on UCH-L1 and UCH-L3 (IC50 > 500 µM).
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number2062-78-4
          Chemical formulaC₂₈H₂₉F₂N₃O
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (50 mg/ml)
          Storage -20°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions ar stable for up to 6 months at -20°C.
          Toxicity Regulatory Review
          ReferencesChen, J., et al. 2011. Chem. Biol 18, 1390.
          Nelson, E.A., et al. 2011. Blood 117, 3421.