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104833 Ack1 Inhibitor, AIM-100 - CAS 873305-35-2 - Calbiochem

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Synonymes: (S)-5,6-Diphenyl-N-((tetrahydrofuran-2-yl)methyl)furo[2,3-d]pyrimidin-4-amine, Activated Cdc42 Kinase 1 Inhibitor

Primary Target: Ack1
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      Aperçu

      Tableau de caractéristiques principal

      CAS #Empirical Formula
      873305-35-2C₂₃H₂₁N₃O₂
      Description
      OverviewA cell-permeable furopyrimidine that acts as a potent, ATP-binding site-targeting, Ack1-selective inhibitor (IC50 = 22 nM) and effectively prevents receptor-mediated Ack1 activation (by >90% in MEF & LAPC4 cultures; 16 h 800 nM), while exhibiting much reduced potency against Lyn, Lck, Abl1 and BTK (IC50 ≥346.7 nM) and no inhibitory activity toward 25 other kinases. Shown to completely inhibit EGF-induced, but not androgen DHT- (dihydrotestosterone) stimulated, AR transcription activity in serum- and androgen-deprived prostate cancer LAPC4 cutlures. Effectively inhibits androgen-independent LNCaP prostate cancer growth both in vitro (by 60%; 72 h 8 µM) and in castrated mice in vivo (4 mg/kg/96 h injections on day 7/11/15/19/23/27 post tumor transplant).
      Catalogue Number104833
      Brand Family Calbiochem®
      Synonyms(S)-5,6-Diphenyl-N-((tetrahydrofuran-2-yl)methyl)furo[2,3-d]pyrimidin-4-amine, Activated Cdc42 Kinase 1 Inhibitor
      References
      ReferencesMahajan, K., et al. 2012. J. Biol. Chem. 287, 22112.
      Mahajan, K., et al. 2012. Am. J. Pathol. 180, 1386.
      Mahajan, K., et al. 2010. Prostate 70, 1274.
      DiMauro, E.F., et al. 2007. Bioorg. Med. Chem. Lett. 17, 2305.
      Product Information
      CAS number873305-35-2
      FormYellow solid
      Hill FormulaC₂₃H₂₁N₃O₂
      Chemical formulaC₂₃H₂₁N₃O₂
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetAck1
      Primary Target IC<sub>50</sub>22 nM for Ack1
      Secondary targetLck, Lyn
      Purity≥98% by Chiral HPLC
      Enantiomeric excess (ee): 98.29% (based on the ee of (S)-(+)-Tetrahydrofurfurylamine, as determined using Chiral HPLC column)
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Avoid freeze/thaw Avoid freeze/thaw
      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
      Global Trade Item Number
      Référence GTIN
      104833 0