528121 PI 3-K/PDK-1 Inhibitor, NVP-BAG956 - CAS 853910-02-8 - Calbiochem

528121
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₈H₂₁N₅ 853910-02-8

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      528121-5MG
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable imidazoquinoline compound that acts as a potent, reversible, and ATP-competitive PI 3-K/PDK1 dual kinase inhibitor (IC50 = 56, 446, 35, 117, and 245 nM against p110α, p110β, p110δ, p110γ, and PDK1, respectively), displaying much reduced potency against VEGFR1 (IC50 = 2.56 µM) and little or no activity toward a panel of 15 other kinases (IC50 >10 µM). Shown to effectively inhibit the constitutive phosphorylation of PKB (T308 & S473; IC50 ≤45 nM) as well as PKB downstream effectors GSK3β (S9), FKHRL1 (T32), and p70S6K (T389) in human glioma U87MG and adeonocarcinoma PC3M cultures with PTEN deletion in vitro and retard PC3M-derived tumor growth in mice (by 50%; 75 mg/kg; twice per day p.o.) in vivo. Also reported to exhibit antiproliferative activities against BCRF-ABL- and mutant FLT3-expressing cells either alone or in combination with other PI3K/AKT, mTOR, and tyrosine kinase inhibitors, LY294002 (Cat. Nos. 440202 & 440204), Rapamycin (Cat. No. 553210), and PKC412 (Cat. No. 539648).
          Catalogue Number528121
          Brand Family Calbiochem®
          Synonymsα,α,-Dimethyl-4-(2-methyl-8-(2-(3-pyridinyl)ethynyl)-1H-imidazo[4,5-c]quinolin-1-yl)-benzeneacetonitrile , BAG956, PI 3-K Inhibitor XVI, PDK1 Inhibitor IV
          References
          ReferencesMarone, R., et al. 2009. Mol. Cancer Res. 7, 601.
          Weisberg, E., et al. 2008. Blood 111, 3723.
          Stauffer, F., et al. 2008. Bioorg. Med. Chem. Lett. 18, 1027.
          Product Information
          CAS number853910-02-8
          FormOrange powder
          Hill FormulaC₂₈H₂₁N₅
          Chemical formulaC₂₈H₂₁N₅
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥98% 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 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          PI 3-K/PDK-1 Inhibitor, NVP-BAG956 - CAS 853910-02-8 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          PI 3-K/PDK-1 Inhibitor, NVP-BAG956 - CAS 853910-02-8 - Calbiochem Certificates of Analysis

          TitleLot Number
          528121

          References

          Reference overview
          Marone, R., et al. 2009. Mol. Cancer Res. 7, 601.
          Weisberg, E., et al. 2008. Blood 111, 3723.
          Stauffer, F., et al. 2008. Bioorg. Med. Chem. Lett. 18, 1027.
          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.

          Revision21-October-2011 RFH
          Synonymsα,α,-Dimethyl-4-(2-methyl-8-(2-(3-pyridinyl)ethynyl)-1H-imidazo[4,5-c]quinolin-1-yl)-benzeneacetonitrile , BAG956, PI 3-K Inhibitor XVI, PDK1 Inhibitor IV
          DescriptionA cell-permeable imidazoquinoline compound that acts as a potent, reversible, and ATP-competitive PI 3-K/PDK1 dual kinase inhibitor (IC50 = 56, 446, 35, 117, and 245 nM against p110α, p110β, p110δ, p110γ, and PDK1, respectively), displaying much reduced potency against VEGFR1 (IC50 = 2.56 µM) and little or no activity toward a panel of 15 other kinases (IC50 >10 µM). Shown to effectively inhibit the constitutive phosphorylation of PKB (T308 & S473; IC50 ≤45 nM) as well as PKB downstream effectors GSK3β (S9), FKHRL1 (T32), and p70S6K (T389) in human glioma U87MG and adeonocarcinoma PC3M cultures with PTEN deletion in vitro and retard PC3M-derived tumor growth in mice (by 50%; 75 mg/kg; twice per day p.o.) in vivo. Also reported to exhibit antiproliferative activities against BCRF-ABL- and mutant FLT3-expressing cells either alone or in combination with other PI3K/AKT, mTOR, and tyrosine kinase inhibitors, LY294002 (Cat. Nos. 440202 & 440204), Rapamycin (Cat. No. 553210), and PKC412 (Cat. No. 539648).
          FormOrange powder
          Intert gas (Yes/No) Packaged under inert gas
          CAS number853910-02-8
          Chemical formulaC₂₈H₂₁N₅
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (25 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 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesMarone, R., et al. 2009. Mol. Cancer Res. 7, 601.
          Weisberg, E., et al. 2008. Blood 111, 3723.
          Stauffer, F., et al. 2008. Bioorg. Med. Chem. Lett. 18, 1027.