189412 Aurora Kinase Inhibitor XI, HOI-07

189412
  
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₁₉H₁₃NO₄
      Description
      OverviewA cell-permeable oxindole compound that selectively inhibits Aurora B, but not Aurora A, activity (IC50 ≤100 nM; [ATP] = 100 µM) and potently suppresses cellular histone H3 Ser10 phosphorylation (IC50 <100 nM in A549 cells; 24 h) by targeting kinase ATP-binding site, exhibiting much reduced potency toward a panel of 49 other kinases (≤53% inhibition at 5 µM). Although noncytotoxic at ≤1 µM, HOI-07 treatment does induce G2/M arrest and apoptosis in A549 culutres at higher concentrations (5 µM). Potently inhibits anchorage-independent growths of human lung and colon cancer lines (by >80% at 0.5 µM) in vitro and is efficacious in suppressing A549 tumor expansion in mice (10, and 20 mg/kg; twice weekly i.p.) in vivo.

      This product has been discontinued.





      Catalogue Number189412
      Brand Family Calbiochem®
      Synonyms(E)-3-((E)-4-(Benzo[d][1,3]dioxol-5-yl)-2-oxobut-3-enylidene)indolin-2-one
      References
      ReferencesXie, H., et al. 2012. Cancer Res. 73, 716.
      Product Information
      FormRed solid
      Hill FormulaC₁₉H₁₃NO₄
      Chemical formulaC₁₉H₁₃NO₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Applications
      Biological Information
      Primary TargetAurora B
      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 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 1 month at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      References

      Reference overview
      Xie, H., et al. 2012. Cancer Res. 73, 716.
      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.

      Revision19-March-2013 JSW
      Synonyms(E)-3-((E)-4-(Benzo[d][1,3]dioxol-5-yl)-2-oxobut-3-enylidene)indolin-2-one
      DescriptionA cell-permeable oxindole compound that selectively inhibits Aurora B, but not Aurora A, activity toward histone H3 Ser10 phosphorylation in cell-free kinase assays (IC50 ≤100 nM; [ATP] = 100 µM; 30 min) and in cultures (IC50 <100 nM in A549 cells; 24 h) by targeting kinase ATP-binding site, exhibiting much reduced or little potency toward a panel of 49 other kinases (≤53% inhibition at 5 µM). Although noncytotoxic at ≤1 µM (48 h; by MTT assay using human lung cancer A549 and non-cancer MRC-5 cells), HOI-07 treatment does induce polyploidy in A549 culutres (1 µM; 48 h), while G2/M arrest (17% without vs. 27% with 48 h 5 µM drug treatment) and apoptosis induction (8.2% without vs. 48.6% with 72 h 5 µM drug treatment) occur at higher drug concentrations. Potently inhibits anchorage-independent growths of human lung and colon cancer lines at noncytotoxic concentrations (82%, 83%, 86%, and 91% inhibition, respectively, of A549, H1650, H520, and HCT116 agar colonies formation by 0.5 µM HOI-07) in vitro and is efficacious in suppressing A549-derived tumor expansion in mice (Av. fold expansion from day 8 to day 31 = 8.2, 5.0, and 3.4 with twice weekly i.p.dosage of 0, 10, and 20 mg/kg, respectively) with concomitant reduction of Ki-67 protein level and histone H3 Ser10 phosphorylation in tumor tissues (by 65% and 72%, respectively) in vivo.
      FormRed solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₉H₁₃NO₄
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (10 mg/ml). Use only fresh DMSO for reconstitution.
      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 1 month at -20°C.
      Toxicity Standard Handling
      ReferencesXie, H., et al. 2012. Cancer Res. 73, 716.