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521276 PDK1 Inhibitor II - CAS 850717-64-5 - Calbiochem

The PDK1 Inhibitor II, also referenced under CAS 850717-64-5, controls the biological activity of PDK1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

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

Synonyms: 2-Oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]indolin-5-yl]urea, BX-517

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521276
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
850717-64-5C₁₅H₁₄N₄O₂

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      Description
      OverviewA cell-permeable indolinone compound that acts as a potent, ATP site-targeting PDK1 inhibitor (IC50 = 6 nM) and effectively suppresses cellular Akt Thr308 phosphorylation level in PC-3 cultures (IC50 ≤1 µM), while affecting PKA (IC50 = 1.6 µM) and 7 other kinases (IC50 ≥600 nM) only at much higher concentrations. Its in vivo applicability is limited by a low aqueous solubility (2 µg/ml in PBS) and poor pharmacokinetics.
      Catalogue Number521276
      Brand Family Calbiochem®
      Synonyms2-Oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]indolin-5-yl]urea, BX-517
      References
      ReferencesIslam, I., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3819.
      Islam, I., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3814.
      Product Information
      CAS number850717-64-5
      FormDark brown solid
      Hill FormulaC₁₅H₁₄N₄O₂
      Chemical formulaC₁₅H₁₄N₄O₂
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% by HPLC (sum of two isomers)
      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 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

      Documentation

      PDK1 Inhibitor II - CAS 850717-64-5 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      PDK1 Inhibitor II - CAS 850717-64-5 - Calbiochem Certificates of Analysis

      TitleLot Number
      521276

      References

      Reference overview
      Islam, I., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3819.
      Islam, I., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3814.
      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.

      Revision18-April-2011 RFH
      Synonyms2-Oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]indolin-5-yl]urea, BX-517
      DescriptionA cell-permeable indolinone compound that acts as a potent, ATP site-targeting PDK1 inhibitor (IC50 = 6 nM) and effectively suppresses cellular Akt Thr308 phosphorylation level in PC-3 cultures (IC50 ≤1 µM), while affecting PKA (IC50 = 1.6 µM) and 7 other kinases (IC50 ≥600 nM) only at much higher concentrations. Its in vivo applicability is limited by a low aqueous solubility (2 µg/ml in PBS) and poor pharmacokinetics.
      FormDark brown solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number850717-64-5
      Chemical formulaC₁₅H₁₄N₄O₂
      Structure formulaStructure formula
      Purity≥95% by HPLC (sum of two isomers)
      SolubilityDMSO (25 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
      ReferencesIslam, I., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3819.
      Islam, I., et al. 2007. Bioorg. Med. Chem. Lett. 17, 3814.