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

104833
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₃H₂₁N₃O₂ 873305-35-2

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      104833-10MG
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          Glass bottle 10 mg
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          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®
          SynonymsActivated Cdc42 Kinase 1 Inhibitor, (S)-5,6-Diphenyl-N-((tetrahydrofuran-2-yl)methyl)furo[2,3-d]pyrimidin-4-amine
          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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          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.
          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.

          Revision22-February-2013 JSW
          SynonymsActivated Cdc42 Kinase 1 Inhibitor, (S)-5,6-Diphenyl-N-((tetrahydrofuran-2-yl)methyl)furo[2,3-d]pyrimidin-4-amine
          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 -20°C
          Protect from light
          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.
          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.