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538001 T-00127-HEV1 - CAS 900874-91-1 - Calbiochem

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      Übersicht

      Replacement Information

      Key Spec Table

      CAS #Empirical Formula
      900874-91-1C₂₂H₂₉N₅O₃
      Description
      Overview

      This product has been discontinued.



      A cell-permeable pyrazolopyrimidinamine derived enviroxime-like compound that displays anti-poliovirus activity with broad specificity for enteroviruses (EC50 = 0.77, 3.38, 2.5, 1.03 & >44 µM for PV, CVB3, HRVM, HCV 1b & HCV 2a, respectively). Dose-dependently inhibits viral RNA replication. Acts as a potent, selective, ATP-competitive and reversible inhibitor of PI4KIIIβ (IC50 = 150 nM) with poor affinity towards PI4KIIIα & PI4KIIα (IC50 = ~75 & ≥100 µM). Shown to cause PI4KIIIβ accumulation and reduce PI4P at the Golgi apparatus. Exhibits low cytotoxicity (CC50 > 50 µM in HeLa cells) and attractive PK profile in mice. PI4KIIIβ Inhibitor I, BF738735 (Cat. No. 533657) is also available.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

      Catalogue Number538001
      Brand Family Calbiochem®
      Synonyms3-(3,4-Dimethoxyphenyl)-2,5-dimethyl-N-(2-morpholinoethyl)pyrazolo[1,5-a]pyrimidin-7-amine, PI4KIIIβ Inhibitor II
      DescriptionT-00127-HEV1
      References
      ReferencesMejdrova, I., et al. 2015. J. Med. Chem. 58, In press.
      Spickler, C., et al. 2013. Antimicrob. Agents Chemother. 57, 3358.
      Sasaki, J., et al. 2012. EMBO J. 31, 754.
      Arita, M., et al. 2011. J. Virol. 85, 2364.
      Product Information
      CAS number900874-91-1
      FormOff-whte solid
      Hill FormulaC₂₂H₂₉N₅O₃
      Chemical formulaC₂₂H₂₉N₅O₃
      ReversibleY
      Quality LevelMQ200
      Applications
      Biological Information
      Primary TargetPI4KIIIβ
      Primary Target IC<sub>50</sub>150 nM for PI4KIII&beta
      Purity≥95% 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 3 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
      538001 0

      Documentation

      T-00127-HEV1 - CAS 900874-91-1 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Mejdrova, I., et al. 2015. J. Med. Chem. 58, In press.
      Spickler, C., et al. 2013. Antimicrob. Agents Chemother. 57, 3358.
      Sasaki, J., et al. 2012. EMBO J. 31, 754.
      Arita, M., et al. 2011. J. Virol. 85, 2364.
      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.

      Revision23-August-2016 JSW
      Synonyms3-(3,4-Dimethoxyphenyl)-2,5-dimethyl-N-(2-morpholinoethyl)pyrazolo[1,5-a]pyrimidin-7-amine, PI4KIIIβ Inhibitor II
      DescriptionA cell-permeable pyrazolopyrimidinamine derived enviroxime-like compound that displays anti-poliovirus activity with broad specificity for enteroviruses (EC50 = 0.77, 3.38, 2.5, 1.03 & >44 µM for PV, CVB3, HRVM, HCV 1b & HCV 2a, respectively). Dose-dependently inhibits viral RNA replication. Acts as a potent, selective, ATP-competitive and reversible inhibitor of PI4KIIIβ (IC50 = 150 nM) with poor affinity towards PI4KIIIα & PI4KIIα (IC50 = ~75 & ≥100 µM). Shown to cause PI4KIIIβ accumulation and reduce PI4P at the Golgi apparatus. Exhibits low cytotoxicity (CC50 > 50 µM in HeLa cells) and attractive PK profile in mice. PI4KIIIβ Inhibitor I, BF738735 (Cat. No. 533657) is also available.
      FormOff-whte solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number900874-91-1
      Chemical formulaC₂₂H₂₉N₅O₃
      Purity≥95% 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
      ReferencesMejdrova, I., et al. 2015. J. Med. Chem. 58, In press.
      Spickler, C., et al. 2013. Antimicrob. Agents Chemother. 57, 3358.
      Sasaki, J., et al. 2012. EMBO J. 31, 754.
      Arita, M., et al. 2011. J. Virol. 85, 2364.