124033 | Akt Inhibitor XVI, AT7867 - Calbiochem

124033
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₂₀H₂₀ClN₃

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      US1124033-10MG
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      Limited AvailabilityLimited Availability
      In Stock 
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable pyrazolo compound that acts as a potent inhibitor against Akt (IC50 = 32, 17, and 47 nM against Akt1, Akt2, and Akt3, respectively), PKA (IC50 = 20 nM), and p70S6K (IC50 = 85 nM) in an ATP-competitive manner (Ki = 18 nM using AKT2), with much reduced potency toward RSK1 (IC50 >100 nM) and a panel of 13 other cellular kinases (IC50 >1 µM). Shown to reduce cellular phosphorylation of GSK-3β (IC50 range from 2.08 to 4.45 µM), S6R, FKHRL1, and inhibit the proliferation of cancer cells exhibiting constitutive Akt pathway activation both in vitro (IC50 range from 0.94 to 11.86 µM) and in mice in vivo (20 mg/kg via i.p. or 90 mg/kg via p.o.).
          Catalogue Number124033
          Brand Family Calbiochem®
          Synonymsp70S6K Inhibitor III, 4-(4-Chlorophenyl)-4-(4-(1H-pyrazol-4-yl)-phenyl)-piperidine, PKA Inhibitor XIV, S6K1 Inhibitor III, Chlorophenyl-pyrazolyl-phenyl-piperidine
          References
          ReferencesGrimshaw, K.M., et al. 2010. Mol. Cancer Ther. 9, 1100.
          Saxty, G., et al. 2007. J. Med. Chem. 50, 2293.
          Product Information
          FormWhite powder
          Hill FormulaC₂₀H₂₀ClN₃
          Chemical formulaC₂₀H₂₀ClN₃
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥99% by HPLC
          Physicochemical Information
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          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
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          References

          Reference overview
          Grimshaw, K.M., et al. 2010. Mol. Cancer Ther. 9, 1100.
          Saxty, G., et al. 2007. J. Med. Chem. 50, 2293.
          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.

          Revision23-May-2013 JSW
          Synonymsp70S6K Inhibitor III, 4-(4-Chlorophenyl)-4-(4-(1H-pyrazol-4-yl)-phenyl)-piperidine, PKA Inhibitor XIV, S6K1 Inhibitor III, Chlorophenyl-pyrazolyl-phenyl-piperidine
          DescriptionA cell-permeable pyrazolo compound that acts as a potent inhibitor against Akt (IC50 = 32, 17, and 47 nM against Akt1, Akt2, and Akt3, respectively), PKA (IC50 = 20 nM), and p70S6K (IC50 = 85 nM) in an ATP-competitive manner (Ki = 18 nM using AKT2), with much reduced activity toward RSK1 (IC50 >100 nM) and a panel of 13 other cellular kinases (IC50 >1 µM), including PDK1, PI 3-Kβ, SGK, GSK-3β, and MEK1. Shown to effectively reduce the phosphorylation levels of GSK-3β, S6R, and FKHRL1 (IC50 range from 2.08 to 4.45 µM against GSK-3β pSer9 level), as well as inhibit the proliferation (IC50 range from 0.94 to 11.86 µM) of cancer cells exhibiting constitutive Akt pathway activation, including the PTEN-deficient MES-SA uterine sarcoma and U87MG glioblastoma cell lines. AT7867 treatments via i.p. or p.o. (20 mg/kg and 90 mg/kg, respectively, once every 3 days) are also reported to result in Akt pathway and tumor growth inhibition in mice bearing MES-SA (~40% of untreated control on day 10 by i.p. or p.o.) or U87MG (~50% of untreated control on day 10 by i.p.) xenograft in vivo.
          FormWhite powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₀H₂₀ClN₃
          Structure formulaStructure formula
          Purity≥99% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage +2°C to +8°C
          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.
          Toxicity Standard Handling
          ReferencesGrimshaw, K.M., et al. 2010. Mol. Cancer Ther. 9, 1100.
          Saxty, G., et al. 2007. J. Med. Chem. 50, 2293.