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533717 GLS1 Inhibitor III, CB-839 - CAS 1439399-58-2 - Calbiochem

Cell-permeable, orally available, potent, selective & non-competitive GLS1 inhibitor. Reduces glutamine consumption & glutamate secretion, and induces apoptosis.

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Synonyme: N-(6-(4-(5-((2-Pyridin-2-ylacetyl)amino)-1,3,4-thiadiazol-2-yl)butyl)pyridazin-3-yl)-2-(3-(trifluoromethoxy)phenyl)acetamide, KGA Inhibitor III, 2-(Pyridin-2-yl)-N-(5-(4-(6-(2-(3-(trifluoromethoxy)phenyl)acetamido)pyridazin-3-yl)butyl)-1,3,4-thiadiazol-2-yl)acetamide, GAC Inhibitor III, Kidney-Type Glutaminase Inhibitor III

Primary Target: GLS1
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533717
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Übersicht

Key Spec Table

CAS #Empirical Formula
1439399-58-2C₂₆H₂₄F₃N₇O₃S

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      Description
      OverviewA cell-permeable, orally available thiadiazolyl-butyl-pyridazinyl compound that acts as a potent, selective, time-dependent, and slowly-reversible (t1/2 = 45 min at 25 °C) inhibitor of glutaminase (IC50 = 45, 23 and 28 nM for rec hu-GAC, KGA and GAC, respectively). The inhibition appears to be non-competitive and allosteric. Exhibits anti-proliferative effects in HCC1806 and MDA-MB-231 triple-negative breast cancer cell lines (IC50 = 49 and 26 nM, respectively), but does not affect the viability of ER+/HER2-T47D cell line. Shown to reduce glutamine consumption (IC50 = 17 nM) and glutamate production (IC50 = 15 nM) rates in HCC1806 cells. Inhibits the growth of HCC1806 xenografts in mice (~200 mg/kg, p.o., b.i.d) and of JIMT-1 xenografts (200 mg/kg p.o., b.i.d), either alone or in combination with paclitaxel (10 mg/kg , 5 doses alternate days).

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533717
      Brand Family Calbiochem®
      SynonymsN-(6-(4-(5-((2-Pyridin-2-ylacetyl)amino)-1,3,4-thiadiazol-2-yl)butyl)pyridazin-3-yl)-2-(3-(trifluoromethoxy)phenyl)acetamide, KGA Inhibitor III, 2-(Pyridin-2-yl)-N-(5-(4-(6-(2-(3-(trifluoromethoxy)phenyl)acetamido)pyridazin-3-yl)butyl)-1,3,4-thiadiazol-2-yl)acetamide, GAC Inhibitor III, Kidney-Type Glutaminase Inhibitor III
      DescriptionGLS1 Inhibitor III, CB-839
      References
      ReferencesGross, M.I., et al. 2014. Mol. Cancer Ther. 13, 890.
      Product Information
      CAS number1439399-58-2
      FormYellow to brown solid
      Hill FormulaC₂₆H₂₄F₃N₇O₃S
      Chemical formulaC₂₆H₂₄F₃N₇O₃S
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetGLS1
      Primary Target IC<sub>50</sub>23 nM & 28 nM, respectively, using murine kidney and brain homogenates
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      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
      Global Trade Item Number
      Bestellnummer GTIN
      5337170001 04055977286656