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526526 PIM3 Kinase Inhibitor VII, M-110 - Calbiochem

SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.

Synonyme: Nʹ-(1-(4-Chloro-2-hydroxyphenyl)propylidene)-2-((3-morpholinopropyl)amino)isonicotinohydrazide

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526526
Preis & Verfügbarkeit

Übersicht

Replacement Information

Key Spec Table

Empirical Formula
C₂₂H₂₈ClN₅O₃

Preis & Verfügbarkeit

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526526-10MG
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      		 Glasflasche 10 mg
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      Description
      OverviewA cell-permeable hydroxyphenyl-propylidene-benzohydrazide compound that acts as a potent, ATP-competitive (Ki = 0.3 µM), and highly isoform-selective PIM inhibitor (IC50 = 2.5, 2.5, and 0.047 µM against PIM1, PIM2, and PIM3, respectively; [ATP] = 10 µM), while affecting CK2α2 only at much higher concentrations (IC50 = 5 µM, [ATP] = 10 µM) and exhibiting little or no activity against a panel of 258 other kinases (<40% inhibition at 5 µM). Shown to inhibit PIM3-dependent STAT3 Tyr705 phosphorylation in DU-145 prostate cancer and MiaPaCa2 pancreatic cancer cells (by 73% and 83%, respectively; 10 µM for 18 h), while displaying little effect toward STAT3 Tyr694 phosphoylation in 22RV1 cultures.
      Catalogue Number526526
      Brand Family Calbiochem®
      SynonymsNʹ-(1-(4-Chloro-2-hydroxyphenyl)propylidene)-2-((3-morpholinopropyl)amino)isonicotinohydrazide
      References
      ReferencesChang, M., et al. 2010. Mol. Cancer Ther. 9, 2478.
      Product Information
      FormPale yellow solid
      Hill FormulaC₂₂H₂₈ClN₅O₃
      Chemical formulaC₂₂H₂₈ClN₅O₃
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥97% 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 Shipped with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      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 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
      Global Trade Item Number
      Bestellnummer GTIN
      526526-10MG 04055977270792

      Documentation

      PIM3 Kinase Inhibitor VII, M-110 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      PIM3 Kinase Inhibitor VII, M-110 - Calbiochem Analysenzertifikate

      TitelChargennummer
      526526

      Literatur

      Übersicht
      Chang, M., et al. 2010. Mol. Cancer Ther. 9, 2478.
      Datenblatt

      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.

      Revision22-February-2013 JSW
      SynonymsNʹ-(1-(4-Chloro-2-hydroxyphenyl)propylidene)-2-((3-morpholinopropyl)amino)isonicotinohydrazide
      DescriptionA cell-permeable hydroxyphenyl-propylidene-benzohydrazide compound that acts as a potent, ATP-competitive (Ki = 0.3 µM), and highly isoform-selective PIM inhibitor (IC50 = 2.5, 2.5, and 0.047 µM against PIM1, PIM2, and PIM3, respectively, with PIMtide as substrate, [ATP] = 10 µM), while affecting CK2α2 only at much higher concentrations (IC50 = 5 µM, [ATP] = 10 µM) and exhibiting little or no activity against a panel of 258 other kinases (<40% inhibition; [M-110] = 5 µM). M-100 treatment (10 µM for 18 hr) is shown to inhibit both basal (by 73% and 83% of DMSO control in DU-145 prostate cancer and MiaPaCa2 pancreatic cancer cells, respectively) and IL-6-stimulated (by 69% of DMSO control in DU-145 cells) STAT3 phosphorylation on Tyr705, while displaying little effect toward Tyr694 phosphoylation (in 22RV1 cultures). Isoform-specific knockdowns in DU-145 cells likewise identify PIM-3, but not PIM-1 or -2, as the kinase responsible for cellular STAT3 Tyr705 phosphorylation.
      FormPale yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₂H₂₈ClN₅O₃
      Structure formulaStructure formula
      Purity≥97% 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 are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesChang, M., et al. 2010. Mol. Cancer Ther. 9, 2478.