528119 | PI 3-K Inhibitor XI, HWT - CAS 58053-83-1 - Calbiochem

528119
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₃H₂₆O₈ 58053-83-1

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      528119-5MG
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          5 mg
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          Description
          OverviewA cell-permeable Wortmannin (Cat. Nos. 681675 and 681676) 17β-Hydroxy analog (HWT) that acts as an irreversible PI 3-K inhibitor with an 8.4-fold higher potency than that of Wortmannin (IC50 = 0.5 and 4.2 nM, respectively) and inhibits mTOR only at much higher concentrations (IC50 = 0.193 µM). Both Wortmannin and HWT covalently modify a conserved lysine residue (Lys833 in porcine PI 3-Kγ) in the PI 3-K ATP binding pocket via their electrophilic furan ring at C-20 position. HWT is shown to effectively arrest the growth of LNCaP cells (IC50 = 1.464 µM) in vitro, however, its high in vivo toxicity renders it unsuitable for tumor killing studies in mice. Also reported to inhibit late phase PLD-mediated PA production upon fMLP (Cat. No. 05-22-2500) stimulation of human neutrophils.
          Catalogue Number528119
          Brand Family Calbiochem®
          SynonymsWortmannin, 17β-Hydroxy, LY 301497, mTOR Inhibitor VIII
          References
          ReferencesZask, A., et al. 2008. J. Med. Chem. 51, 1319.
          Zhu, T., et al. 2006. J. Med. Chem. 49, 1373.
          Norman, B. H., et al. 1996. J. Med. Chem. 39, 1106.
          Gelas, P., et al. 1992. Biochem. J. 287, 67.
          Product Information
          CAS number58053-83-1
          FormOff-white solid
          Hill FormulaC₂₃H₂₆O₈
          Chemical formulaC₂₃H₂₆O₈
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥97% 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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          528119

          References

          Reference overview
          Zask, A., et al. 2008. J. Med. Chem. 51, 1319.
          Zhu, T., et al. 2006. J. Med. Chem. 49, 1373.
          Norman, B. H., et al. 1996. J. Med. Chem. 39, 1106.
          Gelas, P., et al. 1992. Biochem. J. 287, 67.
          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.

          Revision03-December-2010 RFH
          SynonymsWortmannin, 17β-Hydroxy, LY 301497, mTOR Inhibitor VIII
          DescriptionA cell-permeable Wortmannin (Cat. Nos. 681675 and 681676) 17β-Hydroxy analog (HWT) that acts as an irreversible PI 3-K inhibitor with an 8.4-fold higher potency than that of Wortmannin (IC50 = 0.5 and 4.2 nM, respectively) and inhibits mTOR only at much higher concentrations (IC50 = 0.193 µM). Both Wortmannin and HWT covalently modify a conserved lysine residue (Lys833 in porcine PI 3-Kγ) in the PI 3-K ATP binding pocket via their electrophilic furan ring at C-20 position. HWT is shown to effectively arrest the growth of LNCaP cells (IC50 = 1.464 µM) in vitro, however, its high in vivo toxicity renders it unsuitable for tumor killing studies in mice. Also reported to inhibit late phase PLD-mediated PA production upon fMLP (Cat. No. 05-22-2500) stimulation of human neutrophils.
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number58053-83-1
          Chemical formulaC₂₃H₂₆O₈
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (100 mg/ml); Use only fresh DMSO.
          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
          ReferencesZask, A., et al. 2008. J. Med. Chem. 51, 1319.
          Zhu, T., et al. 2006. J. Med. Chem. 49, 1373.
          Norman, B. H., et al. 1996. J. Med. Chem. 39, 1106.
          Gelas, P., et al. 1992. Biochem. J. 287, 67.