204001 BX-795 - CAS 702675-74-9 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₂₃H₂₆IN₇O₂S 702675-74-9

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204001-10MG
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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable aminopyrimidine compound that acts as a potent, ATP-competitive and reversible multi-kinase inhibitor (IC50 = 11 nM for PDK1 at ≤ 10 µM of ATP; IC50 = 5 , 6, 19, 31, 41 and 111 nM for NUAK1, TBK1, MARK4, Aurora B, IKKε and PDK1 at 100 µM of ATP, respectively) and displays 50-fold greater selectivity over Cdk2/E, EGFR, GSK-3β, IR, c-Kit, PKA, PKC, TAK1 and VEGFR. Shown to block PDK1/Akt signaling, induce growth arrest and apoptosis in PC-3 and MDA-468 cells (IC50 = 0.25 and 0.75 µM, respectively); further, inhibit phosphorylation (pSer396), nuclear translocation and transcriptional activity of IRF3 and reduce IFN-β production in stimulated macrophages.
      Catalogue Number204001
      Brand Family Calbiochem®
      SynonymsN-(3-((5-Iodo-4-((3-(2-thienylcarbonyl)amino)propyl)amino)-2-pyrimidinyl)amino)phenyl)-1-pyrrolidinecarboxamide, Aurora Kinase Inhibitor VIII, AMPK Related Kinase 5 Inhibitor I, ARK5 Inhibitor I, NUAK Kinase Inhibitor I, NUAK1 Inhibitor I, SnF1 Like Kinase-1 Inhibitor I
      References
      ReferencesClark, K., et al. 2009. J. Biol. Chem. 284, 14136.
      Tamgumcy, T., et al. 2008. Exp. Cell Res. 314, 2299.
      Feldman, R.I., et al. 2005. J. Biol. Chem. 280, 19867.
      Product Information
      CAS number702675-74-9
      FormPale yellow solid
      Hill FormulaC₂₃H₂₆IN₇O₂S
      Chemical formulaC₂₃H₂₆IN₇O₂S
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% 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 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

      BX-795 - CAS 702675-74-9 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      BX-795 - CAS 702675-74-9 - Calbiochem Certificates of Analysis

      TitleLot Number
      204001

      References

      Reference overview
      Clark, K., et al. 2009. J. Biol. Chem. 284, 14136.
      Tamgumcy, T., et al. 2008. Exp. Cell Res. 314, 2299.
      Feldman, R.I., et al. 2005. J. Biol. Chem. 280, 19867.
      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.

      Revision15-October-2011 RFH
      SynonymsN-(3-((5-Iodo-4-((3-(2-thienylcarbonyl)amino)propyl)amino)-2-pyrimidinyl)amino)phenyl)-1-pyrrolidinecarboxamide, Aurora Kinase Inhibitor VIII, AMPK Related Kinase 5 Inhibitor I, ARK5 Inhibitor I, NUAK Kinase Inhibitor I, NUAK1 Inhibitor I, SnF1 Like Kinase-1 Inhibitor I
      DescriptionA cell-permeable aminopyrimidine compound that acts as a potent, ATP-competitive and reversible multi-kinase inhibitor (IC50 = 11 nM for PDK1 at ≤ 10 µM of ATP; IC50 = 5 , 6, 19, 31, 41 and 111 nM for NUAK1, TBK1, MARK4, Aurora B, IKKε and PDK1 at 100 µM of ATP, respectively) and displays 50-fold greater selectivity over Cdk2/E, EGFR, GSK-3β, IR, c-Kit, PKA, PKC, TAK1 and VEGFR. Shown to block PDK1/Akt signaling, induce growth arrest and apoptosis in PC-3 and MDA-468 cells (IC50 = 0.25 and 0.75 µM, respectively); further, inhibit phosphorylation (pSer396), nuclear translocation and transcriptional activity of IRF3 and reduce IFN-β production in stimulated macrophages.
      FormPale yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number702675-74-9
      Chemical formulaC₂₃H₂₆IN₇O₂S
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesClark, K., et al. 2009. J. Biol. Chem. 284, 14136.
      Tamgumcy, T., et al. 2008. Exp. Cell Res. 314, 2299.
      Feldman, R.I., et al. 2005. J. Biol. Chem. 280, 19867.