504173 MAT2A Inhibitor II, FIDAS-5 - Calbiochem

504173
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₅H₁₃ClFN

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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®
      Synonyms(E)-4-(2-Chloro-6-fluorostyryl)-N-methylaniline, Methionine S-Adenosyltransferase 2A Inhibitor II, FIDAS5
      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
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetMAT2A
      Purity≥97% 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

      MAT2A Inhibitor II, FIDAS-5 - Calbiochem 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.

      Revision18-June-2020 JSW
      Synonyms(E)-4-(2-Chloro-6-fluorostyryl)-N-methylaniline, Methionine S-Adenosyltransferase 2A Inhibitor II, FIDAS5
      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≥97% 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.