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

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

同义词: 1-(1-(4,4-Bis(4-fluorophenyl)butyl)-4-piperidinyl)-1,3-dihydro-2H-benzimidazol-2-one

573110
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概述

Replacement Information

重要规格表

CAS #Empirical Formula
2062-78-4C₂₈H₂₉F₂N₃O

Products

产品目录编号包装 数量 / 包装
573110-100MGCN 玻璃瓶 100 mg
Description
Overview

This product has been discontinued.



A 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
Quality LevelMQ100
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
Global Trade Item Number
产品目录编号 GTIN
573110-100MGCN 04055977265965

Documentation

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

职位

物料安全数据表 (MSDS) 

STAT5 Inhibitor III, Pimozide - CAS 2062-78-4 - Calbiochem 分析证书

标题批号
573110

参考

参考信息概述
Chen, J., et al. 2011. Chem. Biol 18, 1390.
Nelson, E.A., et al. 2011. Blood 117, 3421.

技术信息

标题
JAK/STAT Signaling Research Focus
数据表

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 Protect from light
-20°C
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.