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532605 Aurora A/MYCN Dual Inhibitor, CD532 - CAS 1639009-81-6 - Calbiochem

A cell permeable, highly potent, selective inhibitor of Aurora A (IC₅₀ = 48 nM). Disrupts MYCN-Aurora A complex.

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Synonyme: Aurora A Inhibitor, CD532, MYCN Inhibitor, CD532

Primary Target: Aurora A
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532605
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Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
1639009-81-6C₂₆H₂₅F₃N₈O

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      Description
      OverviewA cell permeable diaminopyrimidine derived compound that acts as a highly potent and selective inhibitor of Aurora A (IC50 = 48 nM). Acts by binding to the hinge region via a pyrazole moiety and stabilizes a DFG-in, inactive conformation of Aurora A. Potentiates the loss of the wild-type MYCN protein by disrupting MYCN-Aurora A complex and allowing its ubiquitination and proteasomal degradation in MYCN-amplified SK-N-BE (2) and Kelly neuroblastoma cells (EC50 = 223 and 146.7 nM, respectively). Causes a loss of S-phase entry of cells and allows their accumulation in both G0/G1 and G2 phases. Shown to be effective in vivo with serum t1/2 = 1.5 h in mice.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number532605
      Brand Family Calbiochem®
      SynonymsAurora A Inhibitor, CD532, MYCN Inhibitor, CD532
      References
      ReferencesLee, J.K., et al. 2016. Cancer Cell. 29, In press.
      Gustafson, W. C., et al. 2014. Cancer Cell. 26, 414.
      Product Information
      CAS number1639009-81-6
      FormTan solid
      Hill FormulaC₂₆H₂₅F₃N₈O
      Chemical formulaC₂₆H₂₅F₃N₈O
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetAurora A
      Primary Target IC<sub>50</sub>48 nM
      Secondary targetMYCN
      Purity≥97% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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
      5.32605.0001 04055977281804

      Documentation

      Aurora A/MYCN Dual Inhibitor, CD532 - CAS 1639009-81-6 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Lee, J.K., et al. 2016. Cancer Cell. 29, In press.
      Gustafson, W. C., et al. 2014. Cancer Cell. 26, 414.

      Technische Informationen

      Titel
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      White Paper: Further considerations of antibody validation and usage.
      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.

      Revision15-March-2015 JSW
      SynonymsAurora A Inhibitor, CD532, MYCN Inhibitor, CD532
      DescriptionA cell permeable diaminopyrimidine derived compound that acts as a highly potent and selective inhibitor of Aurora A (IC50 = 48 nM). Acts by binding to the hinge region via a pyrazole moiety and stabilizes a DFG-in, inactive conformation of Aurora A. Potentiates the loss of the wild-type MYCN protein by disrupting MYCN-Aurora A complex and allowing its ubiquitination and proteasomal degradation in MYCN-amplified SK-N-BE (2) and Kelly neuroblastoma cells (EC50 = 223 and 146.7 nM, respectively). Causes a loss of S-phase entry of cells and allows their accumulation in both G0/G1 and G2 phases. Shown to be effective in vivo with serum t1/2 = 1.5 h in mice.
      FormTan solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1639009-81-6
      Chemical formulaC₂₆H₂₅F₃N₈O
      Purity≥97% 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
      ReferencesLee, J.K., et al. 2016. Cancer Cell. 29, In press.
      Gustafson, W. C., et al. 2014. Cancer Cell. 26, 414.