124018 Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 - CAS 612847-09-3 - Calbiochem

124018
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      Overview

      Replacement Information

      Key Spec Table

      Empirical FormulaCAS #
      C₃₄H₂₉N₇O612847-09-3

      Pricing & Availability

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      US1124018-1MG
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          Plastic ampoule 1 mg
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          US1124018-5MG
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              Glass bottle 5 mg
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              Description
              OverviewA cell-permeable and reversible quinoxaline compound that potently and selectively inhibits Akt1/Akt2 activity (IC50 = 58 nM, 210 nM, and 2.12 µM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition appears to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 µM. Overcomes Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and is shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 both in cultured cells in vitro and in mice in vivo. A 10 mM (1 mg/181 µl) solution of Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 (Cat. No. 124017) in DMSO is also available.
              Catalogue Number124018
              Brand Family Calbiochem®
              Synonyms1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one, Akti-1/2
              References
              ReferencesCalleja, V., et al. 2009. PLoS Biol. 7, e17.
              Logie, L., et al. 2007. Diabetes 56, 228.
              Barnett, S.F., et al. 2005. Biochem. J. 385, 399.
              DeFeo-Jones, D., et al. 2005. Mol. Cancer Ther. 4, 271.
              Zhao, Z., et al. 2005. Bioorg. Med. Chem. Lett. 15, 905.
              Lindsley, C.W., et al. 2005. Bioorg. Med. Chem. Lett. 15, 761.
              Product Information
              CAS number612847-09-3
              ATP CompetitiveN
              FormYellow solid
              Hill FormulaC₃₄H₂₉N₇O
              Chemical formulaC₃₄H₂₉N₇O
              ReversibleY
              Structure formula ImageStructure formula Image
              Applications
              ApplicationAkt Inhibitor VIII, Isozyme-Selective, Akti-1/2, CAS 612847-09-3, is a cell-permeable, reversible & selective inhibitor of Akt1/Akt2 (IC50 = 58 nM and 210 nM for Akt1 & Akt2, respectively),
              Biological Information
              Primary TargetAkt1, Akt2, Akt3
              Primary Target IC<sub>50</sub>58 nM, 210 nM, 2.12 µM against Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays
              Purity≥95% by HPLC
              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 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 (-70°C). Stock solutions are stable for up to 6 months at -70°C.
              Packaging Information
              Packaged under inert gas Packaged under inert gas
              Transport Information
              Supplemental Information
              Specifications

              Documentation

              Certificates of Analysis

              TitleLot Number
              124018

              References

              Reference overview
              Calleja, V., et al. 2009. PLoS Biol. 7, e17.
              Logie, L., et al. 2007. Diabetes 56, 228.
              Barnett, S.F., et al. 2005. Biochem. J. 385, 399.
              DeFeo-Jones, D., et al. 2005. Mol. Cancer Ther. 4, 271.
              Zhao, Z., et al. 2005. Bioorg. Med. Chem. Lett. 15, 905.
              Lindsley, C.W., et al. 2005. Bioorg. Med. Chem. Lett. 15, 761.

              Brochure

              Title
              Akt
              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-September-2012 JSW
              Synonyms1,3-Dihydro-1-(1-((4-(6-phenyl-1H-imidazo[4,5-g]quinoxalin-7-yl)phenyl)methyl)-4-piperidinyl)-2H-benzimidazol-2-one, Akti-1/2
              DescriptionA cell-permeable, reversible, potent, and selective inhibitor of Akt1/Akt2 activity (IC50 = 58 nM, 210 nM, and 2.12 µM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays). The inhibition is reported to be pleckstrin homology (PH) domain-dependent. It does not exhibit any inhibitory effect against PH domain-lacking Akts, or other closely related AGC family kinases, PKA, PKC, and SGK, even at concentrations as high as 50 µM. Overcomes Akt1/Akt2-mediated resistance to chemotherapeutics in tumor cells and is shown to block basal and stimulated phosphorylation/activation of Akt1/Akt2 both in cultured cells in vitro and in mice in vivo.
              FormYellow solid
              Intert gas (Yes/No) Packaged under inert gas
              CAS number612847-09-3
              Chemical formulaC₃₄H₂₉N₇O
              Structure formulaStructure formula
              Purity≥95% by HPLC
              SolubilityDMSO (5 mg/ml)
              Storage +2°C to +8°C
              Protect from light
              Do Not Freeze Ok to freeze
              Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
              Toxicity Standard Handling
              ReferencesCalleja, V., et al. 2009. PLoS Biol. 7, e17.
              Logie, L., et al. 2007. Diabetes 56, 228.
              Barnett, S.F., et al. 2005. Biochem. J. 385, 399.
              DeFeo-Jones, D., et al. 2005. Mol. Cancer Ther. 4, 271.
              Zhao, Z., et al. 2005. Bioorg. Med. Chem. Lett. 15, 905.
              Lindsley, C.W., et al. 2005. Bioorg. Med. Chem. Lett. 15, 761.