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

概述

Replacement Information

重要规格表

CAS #Empirical Formula
612847-09-3C₃₄H₂₉N₇O

价格及供货情况

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124018-5MGCN
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      玻璃瓶 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
      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
      产品目录编号 GTIN
      124018-5MGCN 04055977205718

      Documentation

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

      职位

      物料安全数据表 (MSDS) 

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

      标题批号
      124018

      参考

      参考信息概述
      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.

      小册子

      标题
      Akt

      海报

      标题
      Human Kinome & InhibitorSelect™ Libraries
      数据表

      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.