509266 | Mcl-1 Inhibitor III, UMI-77 - Calbiochem

509266
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₈H₁₄BrNO₅S₂

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.09266.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable, bioavailable hydroxynaphthalenylthioacetate compound that selectively and reversibly binds to the BH3 binding groove of Mcl-1 (Ki = 490 nM) and antagonizes its function by disrupting the heterodimerization of Mcl-1/Bax (IC50 = 1.43 µM) and Mcl-1/Bak in cells. Exhibits high selectivity over other members of the Bcl-2 family (Ki = 5.33, 8.19, 23.83, and 32.99 µM, for A1/Bfl-1, Bcl-w, Bcl-2, and Bcl-xL, respectively). Inhibits the growth of BxPC-3, Panc-1 cells, and Capan-2 cells (IC50 = 3.4, 4.4, and 5.5 µM, respectively) by inducing intrinsic apoptosis as evidenced by cytochrome c release and caspase-3 activation. However, it does not induce apoptosis in normal cells. Blocks the growth of BxPC-3 xenograft in SCID mice (60 mg/kg i.v. for 5 days for 2 weeks) without any cytotoxic effects on surrounding normal tissue. Exhibits desirable microsomal stability (t1/2 = 45 min. in murine models).
          Catalogue Number509266
          Brand Family Calbiochem®
          SynonymsMyeloid Cell Leukemia-1 Inhibitor III, UMI77, 2-(4-(4-Bromophenylsulfonamido)-1-hydroxynaphthalen-2-ylthio)acetic acid, ((4-(((4-Bromophenyl)sulfonyl)amino)-1-hydroxy-2-naphthyl)sulfanyl)acetic acid
          References
          ReferencesAbulwerdi, F., et al. 2014. Mol. Cancer Ther. 13, 565.
          Product Information
          FormOff-white solid
          Hill FormulaC₁₈H₁₄BrNO₅S₂
          ReversibleY
          Applications
          Biological Information
          Primary Targetbinds to the BH3 binding groove of Mcl-1
          Purity≥98% 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
          Abulwerdi, F., et al. 2014. Mol. Cancer Ther. 13, 565.
          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.

          Revision01-March-2016 JSW
          SynonymsMyeloid Cell Leukemia-1 Inhibitor III, UMI77, 2-(4-(4-Bromophenylsulfonamido)-1-hydroxynaphthalen-2-ylthio)acetic acid, ((4-(((4-Bromophenyl)sulfonyl)amino)-1-hydroxy-2-naphthyl)sulfanyl)acetic acid
          DescriptionA cell-permeable hydroxynaphthalenylthioacetate that exhibits Mcl-1-selective affinity (Ki against 2 nM FITC-BID79-99 binding = 490 nM/90 nM MCl-1 & 23.83 µM/60 nM Bcl-2; Ki against 1 nM FAM-BID80-99 binding = 5.33 µM/4 nM A1/Bfl-1; Ki against 2 nM FAM-BID80-99 binding = 8.19 µM/40 nM Bcl-w, 23.83 µM/60 nM Bcl-2, and 32.99 µM/50 nM Bcl-xL), effectively inhibiting Mcl-1 BH3-binding groove-mediated interactions with various binding partners, including Noxa, Bax, and Bak, by simultaneously targeting the groove′s h2 & h3 hydrophobic pockets. Shown to inhibit the proliferation of BxPC-3, Panc-1, and Capan-2 prostate cancer cultures (IC50 = 3.4, 4.4, and 5.5 µM, respectively) via apoptosis induction, while being less potent toward MiaPaca and AsPC-1 lines (IC50 = 12.5 and 16.1 µM, respectively) with high Bcl-xL and low Mcl-1/Bak expression and. Despite its moderate in vitro murine liver microsome stability (t1/2 = 45 mins), daily i.v. injection (60 mg/kg; 5 d/wk) is reported to effectively suppress BxPC-3 tumor expansion in mice in vivo without apparent animal toxicity, although severe weight loss is observed among mice received higher daily MUI-77 i.v. dosage of 80 mg/kg.
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          Purity≥98% 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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesAbulwerdi, F., et al. 2014. Mol. Cancer Ther. 13, 565.