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189412 Aurora Kinase Inhibitor XI, HOI-07

189412
  
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Přehled

Replacement Information

Tabulka spec. kláve

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

Přehled odkazů
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 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 1 month at -20°C.
Toxicity Standard Handling
ReferencesXie, H., et al. 2012. Cancer Res. 73, 716.