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

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Synonyme: (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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      Übersicht

      Replacement Information

      Key Spec Table

      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
      Applications
      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
      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 -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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Bestellnummer GTIN
      104833 0

      Documentation

      Literatur

      Übersicht
      Mahajan, 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.
      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.

      Revision22-February-2013 JSW
      Synonyms(S)-5,6-Diphenyl-N-((tetrahydrofuran-2-yl)methyl)furo[2,3-d]pyrimidin-4-amine, Activated Cdc42 Kinase 1 Inhibitor
      DescriptionA 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 (>90% of 10 ng/mL EGF-induced Ack1 Tyr284 phosphorylation in MEF and LAPC4 cells with 16 h 800 nM inhibitor pretreatment), while exhibiting much reduced potency against Lyn, Lck, Abl1 and BTK (IC50 = 346.7, 432.3, 705.9 and 871.7 nM, respectively) and no inhibitory activity toward 25 other kinases. Shown to completely inhibit EGF-induced, but not androgen DHT (dihydrotestosterone)-stimulated, AR (androgen receptor) transcription activity in serum- and androgen-deprived prostate cancer LAPC4 cutlures by preventing Ack1 activation-dependent AR Tyr267 phosphorylation. Effectively inhibits androgen-independent prostate cancer growth both in vitro (by 60% in 72 h 8 µM-treated LNCaP and 108 h 4 µM-treated LAPC4 cultures) and in castrated mice in vivo (18% and 51% of control tumor size on day 27, respectively, of irradiated and non-irradiated active Ack1-expressing LNCaP; Six 4 mg/kg/96 h injections on day 7/11/15/19/23/27 post tumor transplant).
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number873305-35-2
      Chemical formulaC₂₃H₂₁N₃O₂
      Purity≥98% by Chiral HPLC
      Enantiomeric excess (ee): 98.29% (based on the ee of (S)-(+)-Tetrahydrofurfurylamine, as determined using Chiral HPLC column)
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      Avoid freeze/thaw
      -20°C
      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
      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.