260962 DNA-PK Inhibitor III - CAS 404009-40-1 - Calbiochem

260962
Price could not be retrieved
Minimum Quantity needs to be mulitiple of
Upon Order Completion More Information
You Saved ()
 
Request Pricing
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      Contact Customer Service
      View Pricing & Availability
      Click To Print This Page

      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₂H₁₅NO₃ 404009-40-1

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      260962-1MG
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          Contact Customer Service
          Contact Customer Service

          Plastic ampoule 1 mg
          Retrieving price...
          Price could not be retrieved
          Minimum Quantity needs to be mulitiple of
          Upon Order Completion More Information
          You Saved ()
           
          Request Pricing
          Description
          OverviewA cell-permeable aryl-morpholino compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 120 nM) and PI 3-Kinase catalytic subunit p110β (IC50 = 135 nM). It inhibits DNA-PK-mediated cellular DNA DSB (double strand break) repair (EC50 = 68 µM) and enhances DSB-induced antitumor activity both in vitro and in vivo, while exhibiting no cytotoxic effects (up to 50 µM) in the absence of DSBs. It inhibits PI 3-K p110α, p110γ, and p110δ only at much higher concentrations (IC50 = 1.4, 0.88, and 1.0 µM, respectively) and exhibits no effect against a panel of several other kinases, including, Cdk2, Src, PKA, PKC, Chk1, CK1, ATM, and FKBP12, even at concentrations as high as 100 µM.
          Catalogue Number260962
          Brand Family Calbiochem®
          SynonymsIC86621, 1-(2-Hydroxy-4-morpholin-4-yl-phenyl)ethanone
          References
          ReferencesKashishian, A., et al. 2004. Mol. Cancer Ther. 2, 1257.
          Willmore, E., et al. 2004. Blood,103, 4659.
          Product Information
          CAS number404009-40-1
          ATP CompetitiveY
          FormOff-white solid
          Hill FormulaC₁₂H₁₅NO₃
          Chemical formulaC₁₂H₁₅NO₃
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetDNA-PK
          Primary Target IC<sub>50</sub>120 nM against DNA-PK
          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 Ambient Temperature Only
          Toxicity Carcinogenic / Teratogenic
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          260962

          References

          Reference overview
          Kashishian, A., et al. 2004. Mol. Cancer Ther. 2, 1257.
          Willmore, E., et al. 2004. Blood,103, 4659.

          Brochure

          Title
          Akt Brochure
          Biologics 33.1 ( 1.37 MB )
          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.

          Revision04-January-2010 RFH
          SynonymsIC86621, 1-(2-Hydroxy-4-morpholin-4-yl-phenyl)ethanone
          DescriptionA cell-permeable, potent, selective, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 0.12 µM) and the PI-3 kinase catalytic subunit p110β (IC50 = 0.135 µM). It inhibits DNA-PK-mediated cellular DNA DSB (double strand break) repair (EC50 = 68 µM) and enhances DSB-induced anti-tumor activity both in vitro and in vivo. Exhibits no cytotoxic effects (up to 50 µM) in the absence of DSBs. It inhibits PI3K p110α, p110γ, and p110δ only at much higher concentrations (IC50 = 1.4 µM, 880 nM, and 1 µM, respectively) and does not inhibit a panel of several other kinases, including, Cdk2, Src, PKA, PKC, Chk1, CK1, ATM, and FKBP12, even at concentrations as high as 100 µM.
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number404009-40-1
          Chemical formulaC₁₂H₁₅NO₃
          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 (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Toxicity Carcinogenic / Teratogenic
          ReferencesKashishian, A., et al. 2004. Mol. Cancer Ther. 2, 1257.
          Willmore, E., et al. 2004. Blood,103, 4659.