508053 | Mcl-1 Inhibitor II - Calbiochem

508053
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₃H₂₄F₃N₃O

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.08053.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable hydroxynaphthalenylthioacetate that targets Mcl-1 BH3-binding groove and selectively competes against 8 nM FITC-AHA-BIM142-161 for Mcl-1, but not Bcl-xL, binding (IC50 = 310 nM vs >40 µM; [Mcl-1] & [Bcl-xL] = 6.25 nM), displaying little inhibitory potency toward CYP450 isoforms 1A2/2D6/3A4/2C9 (IC50 = >10 µM). Antiproliferation potencies against 2 murine lymphoma cell lines (GI50 = 300 nM/ MCl1-1780 & 1.1 µM/Bcl2-1863) and 11 human cancer lines of various origins (GI50 from 1.6 to 25 µM) correlate well with intracellular BH3 domain peptide-binding capacity. Likewise, greater apoptosis induction is observed in MCl1-1780 than the highly Bcl-2/Bcl-xL primed Bcl2-1863 cultures upon drug treatment. Stability studies using murine and human liver microsome preparations reveal t1/2 values of 40 min and 55 min, respectively.
          Catalogue Number508053
          Brand Family Calbiochem®
          Synonyms7-((4-Ethylpiperazin-1-yl)(4-(trifluoromethyl)phenyl)methyl)quinolin-8-ol, Myeloid Cell Leukemia-1 Inhibitor II
          References
          ReferencesRichard, D.J., et al. 2013. Bioorg. Med. Chem. 21, 6642.
          Product Information
          FormWhite powder
          Hill FormulaC₂₃H₂₄F₃N₃O
          Chemical formulaC₂₃H₂₄F₃N₃O
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetMcl-1
          Purity≥95% 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 6 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) 

          References

          Reference overview
          Richard, D.J., et al. 2013. Bioorg. Med. Chem. 21, 6642.
          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.

          Revision18-December-2013 JSW
          Synonyms7-((4-Ethylpiperazin-1-yl)(4-(trifluoromethyl)phenyl)methyl)quinolin-8-ol, Myeloid Cell Leukemia-1 Inhibitor II
          DescriptionA cell-permeable hydroxynaphthalenylthioacetate that targets Mcl-1 BH3-binding groove and selectively competes against 8 nM FITC-AHA-BIM142-161 for Mcl-1, but not Bcl-xL, binding (IC50 = 310 nM vs >40 µM; [Mcl-1] & [Bcl-xL] = 6.25 nM). Antiproliferation potencies against 2 murine lymphoma cell lines and 11 human cancer lines of various origins (GI50 from 0.3 to 25 µM) correlate well with intracellular BH3 domain peptide-binding capacity. Likewise, greater apoptosis induction is observed in MCl1-1780 than the highly Bcl-2/Bcl-xL primed Bcl2-1863 cultures upon drug treatment.
          FormWhite powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₃H₂₄F₃N₃O
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (25 mg/ml)
          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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesRichard, D.J., et al. 2013. Bioorg. Med. Chem. 21, 6642.