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420099 | JAK Inhibitor I - CAS 457081-03-7 - Calbiochem

420099
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₈H₁₆FN₃O 457081-03-7

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      420099-1MG
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          Glass bottle 1 mg
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          420099-500UG
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              Glass bottle 500 μg
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              Description
              OverviewA potent, reversible, cell-permeable, and ATP-competitive inhibitor of Janus protein tyrosine kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC50 = 15 nM for murine JAK1), JAK2 (IC50 = 1 nM), JAK3 (Ki = 5 nM), and Tyk2 (IC50 = 1 nM). Inhibits other kinases at much higher concentrations. Shown to inhibit IL2- and IL4-dependent proliferation of CTLL cells and block the phosphorylation of STAT5; and further induce growth inhibition of multiple myeloma cells expressing activated JAKs and STAT3, unlike AG 490 (Cat. No. 658401). A 10 mM (500 µg/162 µl) solution of JAK Inhibitor I (Cat. No. 420097) in DMSO is also available.
              Catalogue Number420099
              Brand Family Calbiochem®
              Synonyms2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, Pyridone 6, P6, DBI, JAK1 Inhibitor I, JAK2 Inhibitor I, JAK3 Inhibitor X
              References
              ReferencesPedranzini, L., et al. 2006. Cancer Res. 66, 9714.
              Lucet, I.S., et al. 2005. Blood 107, 176.
              Thompson, J.E., et al. 2002. Bioorg. Med. Chem. Lett. 12, 1219.
              Product Information
              CAS number457081-03-7
              ATP CompetitiveY
              FormOff-white solid
              Hill FormulaC₁₈H₁₆FN₃O
              Chemical formulaC₁₈H₁₆FN₃O
              ReversibleY
              Structure formula Image
              Applications
              Biological Information
              Primary Targetmurine JAK1
              Primary Target IC<sub>50</sub>15 nM against murine JAK1; 1 nM against JAK2; 1 nM against Tyk2
              Primary Target K<sub>i</sub>5 nM against JAK3
              Purity≥98% 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
              420099

              References

              Reference overview
              Pedranzini, L., et al. 2006. Cancer Res. 66, 9714.
              Lucet, I.S., et al. 2005. Blood 107, 176.
              Thompson, J.E., et al. 2002. Bioorg. Med. Chem. Lett. 12, 1219.

              Technical Info

              Title
              JAK/STAT Signaling Research Focus

              Citations

              Title
            • Phuong Thi Nguyen Sarkis, et al. (2006) STAT1-independent cell type-specific regulation of antiviral APOBEC3G by IFN-α. Journal of Immunology 177, 4530-4540.
            • 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.

              Revision12-January-2010 RFH
              Synonyms2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, Pyridone 6, P6, DBI, JAK1 Inhibitor I, JAK2 Inhibitor I, JAK3 Inhibitor X
              DescriptionA potent, cell-permeable, reversible, and ATP-competitive inhibitor of Janus protein tyrosine kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC50 = 15 nM for murine JAK1), JAK2 (IC50 = 1 nM), JAK3 (Ki = 5 nM), and Tyk2 (IC50 = 1 nM). Inhibits other kinases at much higher concentrations. Shown to inhibit IL2- and IL4-dependent proliferation of CTLL cells and block the phosphorylation of STAT5, and further induce growth inhibition of multiple myeloma cells expressing activated JAKs and STAT3, unlike AG 490 (Cat. No. 658401).
              FormOff-white solid
              Intert gas (Yes/No) Packaged under inert gas
              CAS number457081-03-7
              Chemical formulaC₁₈H₁₆FN₃O
              Structure formula
              Purity≥98% by HPLC
              SolubilityDMSO (5 mg/ml)
              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
              ReferencesPedranzini, L., et al. 2006. Cancer Res. 66, 9714.
              Lucet, I.S., et al. 2005. Blood 107, 176.
              Thompson, J.E., et al. 2002. Bioorg. Med. Chem. Lett. 12, 1219.
              Citation
            • Phuong Thi Nguyen Sarkis, et al. (2006) STAT1-independent cell type-specific regulation of antiviral APOBEC3G by IFN-α. Journal of Immunology 177, 4530-4540.