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

Descripción

Replacement Information

Tabla espec. clave

CAS #Empirical Formula
612847-09-3C₃₄H₂₉N₇O

Precios y disponibilidad

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124018-1MG
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      Ampolla de plást. 1 mg
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      124018-5MG
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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
          Quality LevelMQ200
          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
          Global Trade Item Number
          Número de referencia GTIN
          124018-1MG 07790788048006
          124018-5MG 04055977205718

          Documentation

          Licencias necesarias

          Título
          CARTA DE USO GENERAL 2016
          PRODUCTO REGULADO POR LA SECRETARÍA DE SALUD

          Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 - CAS 612847-09-3 - Calbiochem Ficha datos de seguridad (MSDS)

          Título

          Ficha técnica de seguridad del material (MSDS) 

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

          CargoNúmero de lote
          124018

          Referencias bibliográficas

          Visión general referencias
          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.

          Folleto

          Cargo
          Akt

          Póster

          Cargo
          Human Kinome & InhibitorSelect™ Libraries
          Ficha técnica

          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 Protect from light
          +2°C to +8°C
          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.