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324680 Ellipticine, 9-Hydroxy-, Hydrochloride

324680
  
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      Overview

      Replacement Information
      Description
      OverviewA cell-permeable antitumor alkaloid that acts as a potent inhibitor of topoisomerase II (IC50 = 3.3 µM). Restores functional wild-type p53 activity via inhibition of mutant p53 protein phosphorylation. Suppresses Cdk2 activity in a concentration-dependent manner. Also reported to inhibit telomerase activity in cultured pancreatic cells, possibly through inhibition of protein kinases. Binds to the aryl hydrocarbon receptor (AhR) in rat lung cytosol and inhibits aryl hydrocarbon hydroxylase (AHH) activity in rat hepatic microsomes.
      Catalogue Number324680
      Brand Family Calbiochem®
      Synonyms9-HE, HCl
      References
      ReferencesMizumoto, K., et al. 2000. Cancer Lett. 149, 85. Perry, P.J., et al. 1999. Anticancer Drug Des. 14, 373. Sugikawa, E., et al. 1999. Anticancer Res. 19, 3099. Sato, N., et al. 1998. FEBS Lett. 441, 318. Ohashi, M., et al. 1995. Jpn. J. Cancer Res. 86, 819. Renault, G., et al. 1987. Toxicol. Appl. Pharmacol. 89, 281.
      Product Information
      CAS number52238-35-4
      FormBrown solid
      Hill FormulaC₁₇H₁₄N₂O · HCl
      Chemical formulaC₁₇H₁₄N₂O · HCl
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Applications
      Biological Information
      Primary Targettopoisomerase 2
      Primary Target IC<sub>50</sub>3.3 µM
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      R PhraseR: 23/24/25-40

      Toxic by inhalation, in contact with skin and if swallowed.
      Limited evidence of a carcinogenic effect.
      S PhraseS: 36/37/39-45

      Wear suitable protective clothing, gloves and eye/face protection.
      In case of accident or if you feel unwell, seek medical advice immediately (show the label where possible).
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Toxic & Carcinogenic / Teratogenic
      Hazardous Materials Attention: Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.
      Storage -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution in water, aliquot and freeze (-20°C). Aqueous stock solutions are stable for up to 6 months at -20°C. PBS stock solutions are unstable; reconstitute just prior to use.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      324680 0

      Documentation

      Ellipticine, 9-Hydroxy-, Hydrochloride Certificates of Analysis

      TitleLot Number
      324680

      References

      Reference overview
      Mizumoto, K., et al. 2000. Cancer Lett. 149, 85. Perry, P.J., et al. 1999. Anticancer Drug Des. 14, 373. Sugikawa, E., et al. 1999. Anticancer Res. 19, 3099. Sato, N., et al. 1998. FEBS Lett. 441, 318. Ohashi, M., et al. 1995. Jpn. J. Cancer Res. 86, 819. Renault, G., et al. 1987. Toxicol. Appl. Pharmacol. 89, 281.
      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.

      Revision07-April-2008 RFH
      Synonyms9-HE, HCl
      DescriptionA cell-permeable, antitumor alkaloid that acts as a potent inhibitor of topoisomerase II(IC50 = 3.3 µM). Restores functional wild-type p53 activity via inhibition of mutant p53 protein phosphorylation. Shown to induce apoptosis in Saos-2 osteosarcoma cells by arresting cells at G1 stage of the cell cycle. Suppresses Cdk2 activity in a concentration-dependent manner. Also reported to inhibit telomerase activity in cultured pancreatic cancer cells, in a time- and concentration-dependent manner, possibly through inhibition of protein kinases. Binds to the aryl hydrocarbon receptor (AhR) in rat lung cytosol and inhibits aryl hydrocarbon hydroxylase (AHH) activity in rat hepatic microsomes.
      FormBrown solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number52238-35-4
      Chemical formulaC₁₇H₁₄N₂O · HCl
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityPBS or H₂O
      Storage Protect from light
      -20°C
      Hygroscopic
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution in water, aliquot and freeze (-20°C). Aqueous stock solutions are stable for up to 6 months at -20°C. PBS stock solutions are unstable; reconstitute just prior to use.
      Toxicity Toxic & Carcinogenic / Teratogenic
      ReferencesMizumoto, K., et al. 2000. Cancer Lett. 149, 85. Perry, P.J., et al. 1999. Anticancer Drug Des. 14, 373. Sugikawa, E., et al. 1999. Anticancer Res. 19, 3099. Sato, N., et al. 1998. FEBS Lett. 441, 318. Ohashi, M., et al. 1995. Jpn. J. Cancer Res. 86, 819. Renault, G., et al. 1987. Toxicol. Appl. Pharmacol. 89, 281.