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528100 PI-103 - CAS 371935-74-9 - Calbiochem

A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR.

PI-103 - CAS 371935-74-9 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 3-(4-(4-Morpholinyl)pyrido[3ʹ,2ʹ:4,5]furo[3,2-d]pyrimidin-2-yl)phenol, mTOR Inhibitor V, PI 3-K Inhibitor V

Primary Target: DNA-PK, PI3-K, and mTOR
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528100
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
371935-74-9C₁₉H₁₆N₄O₃

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528100-1MGCN
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      528100-5MGCN
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          Description
          OverviewA cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR (IC50 = 2, 8, 88, 48, 150, 26, 20, and 83 nM for DNA-PK, p110α, p110β, p110δ, p110γ, PI3-KC2β, mTORC1, and mTORC2, respectively). It inhibits ATR and ATM only at much higher concentrations (IC50 = 850 and 920 nM, respectively) and exhibits little activity towards a panel of more than 40 other kinases even at concentrations as high as 10 µM. Shown to effectively block PI3-K/Akt signaling and cell proliferation in glioma cell lines both in vitro and in vivo. A 10 mM (2 mg/574 µl) solution of PI-103 (Cat. No. 528101) in DMSO is also available.
          Catalogue Number528100
          Brand Family Calbiochem®
          Synonyms3-(4-(4-Morpholinyl)pyrido[3ʹ,2ʹ:4,5]furo[3,2-d]pyrimidin-2-yl)phenol, mTOR Inhibitor V, PI 3-K Inhibitor V
          References
          ReferencesRaynaud, F.I., et al. 2007. Cancer Res. 67, 5840.
          Fan, Q.W., et al. 2006. Cancer Cell 9, 341.
          Knight, Z.A., et al. 2006. Cell 125, 733.
          Product Information
          CAS number371935-74-9
          ATP CompetitiveY
          FormWhite solid
          Hill FormulaC₁₉H₁₆N₄O₃
          Chemical formulaC₁₉H₁₆N₄O₃
          ReversibleN
          Structure formula ImageStructure formula Image
          Quality LevelMQ100
          Applications
          Biological Information
          Primary TargetDNA-PK, PI3-K, and mTOR
          Primary Target IC<sub>50</sub>2, 8, 88, 48, 150, 26, 20, and 83 nM for DNA-PK, p110α, p110β, p110delta;, p110γ, PI3-KC2β, mTORC1, and mTORC2, respectively
          Purity≥97% 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 Standard Handling
          Storage -20°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
          Global Trade Item Number
          Catalogue Number GTIN
          528100-1MGCN 04055977270457
          528100-5MGCN 04055977270464

          Documentation

          PI-103 - CAS 371935-74-9 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          PI-103 - CAS 371935-74-9 - Calbiochem Certificates of Analysis

          TitleLot Number
          528100

          References

          Reference overview
          Raynaud, F.I., et al. 2007. Cancer Res. 67, 5840.
          Fan, Q.W., et al. 2006. Cancer Cell 9, 341.
          Knight, Z.A., et al. 2006. Cell 125, 733.

          Posters

          Title
          Human Kinome & InhibitorSelect™ Libraries
          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.

          Revision13-October-2010 RFH
          Synonyms3-(4-(4-Morpholinyl)pyrido[3ʹ,2ʹ:4,5]furo[3,2-d]pyrimidin-2-yl)phenol, mTOR Inhibitor V, PI 3-K Inhibitor V
          DescriptionA cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP-competitive inhibitor of DNA-PK, PI3-K, and mTOR (IC50 = 2, 8, 88, 48, 150, 26, 20, and 83 nM for DNA-PK, p110α, p110β, p110δ, p110γ, PI3-KC2β, mTORC1, and mTORC2, respectively). It inhibits ATR and ATM only at much higher concentrations (IC50 = 850 and 920 nM, respectively) and exhibits little activity towards a panel of more than 40 other kinases even at concentrations as high as 10 µM. Shown to effectively block PI3-K/Akt signaling and cell proliferation in glioma cell lines both in vitro and in vivo.
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number371935-74-9
          Chemical formulaC₁₉H₁₆N₄O₃
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (5 mg/ml). Slight warming may be required for complete solubilization.
          Storage Protect from light
          -20°C
          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 Standard Handling
          ReferencesRaynaud, F.I., et al. 2007. Cancer Res. 67, 5840.
          Fan, Q.W., et al. 2006. Cancer Cell 9, 341.
          Knight, Z.A., et al. 2006. Cell 125, 733.