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

528100
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₉H₁₆N₄O₃ 371935-74-9

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      528100-1MG
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          Plastic ampoule 1 mg
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          528100-5MG
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              Plastic ampoule 5 mg
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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, PI 3-K Inhibitor V, mTOR 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
              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

              Documentation

              SDS

              Title

              Safety Data Sheet (SDS) 

              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.
              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, PI 3-K Inhibitor V, mTOR 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 -20°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 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.