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410972 IDH1 Inhibitor, R132 Somatic Mutant-Specific, AGI-5198 - CAS 1355326-35-0 - Calbiochem

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Synonyme: N-Cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-methyl-1H-imidazol-1-yl)acetamido)-2-(o-tolyl)acetamide, HCl, AGI-5198, AGI-5198, Isocitrate Dehydrogenase 1 R132 Somatic Mutant Inhibitor, AGI-5198

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      Übersicht

      Replacement Information
      Description
      Overview

      This product has been discontinued.



      A cell-permeable phenyl-glycine analog that acts as an IDH1 (Isocitrate Dehydrogenase 1) R132 somatic mutant-specific inhibitor (IC50 = 0.07, 0.16, and >100 µM, respectively, against R132H, R132C, and wt IDH1), potently inhibiting oncometabolite 2-HG (D-2-hydroxyglutarate) production, but not cancer viability, in R132H-harboring U87-MG glioblastoma and R132C-harboring HT1080 chondrosarcoma cultures in vitro (IC50 = 70 and 480 nM, respectively; 48 h) and in R132H U87-MG tumor-bearing mice in vivo (150 mg/kg/12 h i.p.). Oncometabolite 2-HG acts as an α-KG-competitive inhibitor against multiple α-KG-dependent enzymes that are important in maintaining normal cellular functions, including epigenetic regulations.
      Catalogue Number410972
      Brand Family Calbiochem®
      SynonymsN-Cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-methyl-1H-imidazol-1-yl)acetamido)-2-(o-tolyl)acetamide, HCl, AGI-5198, AGI-5198, Isocitrate Dehydrogenase 1 R132 Somatic Mutant Inhibitor, AGI-5198
      References
      ReferencesRohle, D., et al. 2013. Science 340, 626.
      Popovici-Muller, J., et al. 2012. ACS Med. Chem. Lett. 3, 850.
      Product Information
      CAS number1355326-35-0
      FormOff-white powder
      Hill FormulaC₂₇H₃₁FN₄O₂ • HCl
      Chemical formulaC₂₇H₃₁FN₄O₂ • HCl
      Hygroscopic Hygroscopic
      ReversibleY
      Structure formula ImageStructure formula Image
      Applications
      Biological Information
      Primary Targetactive site IDH1 mutant homodimer
      Primary Target IC<sub>50</sub>0.07, 0.16, and >
      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
      Hygroscopic Hygroscopic
      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
      Global Trade Item Number
      Bestellnummer GTIN
      410972 0

      Documentation

      IDH1 Inhibitor, R132 Somatic Mutant-Specific, AGI-5198 - CAS 1355326-35-0 - Calbiochem Analysenzertifikate

      TitelChargennummer
      410972

      Literatur

      Übersicht
      Rohle, D., et al. 2013. Science 340, 626.
      Popovici-Muller, J., et al. 2012. ACS Med. Chem. Lett. 3, 850.
      Datenblatt

      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.

      Revision06-September-2013 JSW
      SynonymsN-Cyclohexyl-2-(N-(3-fluorophenyl)-2-(2-methyl-1H-imidazol-1-yl)acetamido)-2-(o-tolyl)acetamide, HCl, AGI-5198, AGI-5198, Isocitrate Dehydrogenase 1 R132 Somatic Mutant Inhibitor, AGI-5198
      DescriptionA cell-permeable phenyl-glycine analog that acts as an IDH1 (Isocitrate Dehydrogenase 1) R132 somatic mutant-specific inhibitor (IC50 = 0.07, 0.16, and >100 µM, respectively, against R132H, R132C, and wt IDH1) and potently inhibits R132 somatic mutant-catalyzed α-KG (α-ketoglutarate) to 2-HG (D-2-hydroxyglutarate) conversion in R132H-harboring U87-MG glioblastoma and R132C-harboring HT1080 chondrosarcoma cultures (IC50 = 70 and 480 nM, respectively; 48 h), without interfering with cell growth (GI50 > 20 µM; 72 h in R132 mutant-harboring HT1080 and U87-MG cutlures) or wild-type enzyme-catalyzed α-KG production. Shown to suppresses R132H U87-MG tumor 2-HG production in mice in vivo albeit that a frequent and heavy i.p. dosing regiment (max inhibtion = 89% at 4 h after three 150 mg/kg/12 h i.p. dosings) is needed to maintain effective free inhibitor concentration in plasma. Oncometabolite 2-HG acts as an α-KG-competitive inhibitor against multiple α-KG-dependent enzymes that are important in maintaining normal cellular functions, including epigenetic regulations.
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1355326-35-0
      Chemical formulaC₂₇H₃₁FN₄O₂ • HCl
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml) or H₂O (2.5 mg/mL)
      Storage Protect from light
      +2°C to +8°C
      Hygroscopic
      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
      ReferencesRohle, D., et al. 2013. Science 340, 626.
      Popovici-Muller, J., et al. 2012. ACS Med. Chem. Lett. 3, 850.