504173 | MAT2A Inhibitor II, FIDAS-5 - Calbiochem

504173
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₅H₁₃ClFN

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.04173.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable fluorinated N,N-dialkylaminostilbene (FIDAS) analogue of FIDAS-3 (Cat. No. 681677) that competes against SAM for MAT2A binding and is >2-fold more potent than FIDAS-3 in inhibiting MAT2A-catalyzed SAM synthesis both in cell-free assays (IC50 = 2.1 µM) and in LS174T colorectal cancer (CRC) cultures (3 µM). FIDAS-5 at 3 µM is shown to completely inhibit the proliferation of LS174T for up to 7 d in vitro and effectively suppress HT29 CRC tumor expansion in mice in vivo (20 mg/kg/day p.o.).
          Catalogue Number504173
          Brand Family Calbiochem®
          SynonymsMethionine S-Adenosyltransferase 2A Inhibitor II, FIDAS5, (E)-4-(2-Chloro-6-fluorostyryl)-N-methylaniline
          References
          ReferencesZhang, W., et al. 2013. ACS Chem. Biol. 8, 796.
          Product Information
          FormYellow semi-solid
          Hill FormulaC₁₅H₁₃ClFN
          Chemical formulaC₁₅H₁₃ClFN
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetMAT2A
          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 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) 

          References

          Reference overview
          Zhang, W., et al. 2013. ACS Chem. Biol. 8, 796.
          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.

          Revision20-September-2013 JSW
          SynonymsMethionine S-Adenosyltransferase 2A Inhibitor II, FIDAS5, (E)-4-(2-Chloro-6-fluorostyryl)-N-methylaniline
          DescriptionA cell-permeable fluorinated N,N-dialkylaminostilbene (FIDAS) analogue of FIDAS-3 (Cat. No. 681677) that is >2-fold more potent than FIDAS-3 in inhibiting MAT2A-catalyzed SAM (S-adenosylmethionine) synthesis both in cell-free (IC50 = 2.1 µM with FIDAS-5 vs. 4.9 µM with FIDAS-3; [L-Met] = [ATP] = 1 mM, [MAT2A] = 10 µg/mL; 20 min FIDAS preincubation prior to 30 min reaction) and cell-based (64% and 56% decrease of SAM and SAH level, respectively, in LS174T cells after 36 h treatment with either 3 µM FIDAS-5 or 10 µM FIDAS-3) assays. FIDAS-5 at 3 µM is shown to completely inhibit the proliferation of LS174T CRC (colorectal cancer) for up to 7 d in vitro and, when administered orally, effectively suppress HT29 CRC tumor expansion in mice in vivo (by 58% on d 18 post HT29 xenograft; 20 mg/kg/day starting d 4). Computer-aided in silico modeling predicts that FIDAS-3 & -5 target SAM-binding pocket at the interface of MAT2A dimer and in vitro binding studies reveals FIDAS-3 effectively competes against SAM for MAT2A binding.
          FormYellow semi-solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₅H₁₃ClFN
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (100 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesZhang, W., et al. 2013. ACS Chem. Biol. 8, 796.