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

JAK Inhibitor I, CAS 457081-03-7, is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK 1 (IC₅₀ = 15 nM), JAK2 (IC₅₀ = 1 nM), JAK3 (Ki = 5 nM) and Tyk2 (IC₅₀ = 1 nM).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 2-(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

Primary Target: murine JAK1
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420099
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
457081-03-7C₁₈H₁₆FN₃O

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420099-1MGCN
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      420099-500UGCN
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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 ImageStructure formula Image
          Quality LevelMQ100
          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
          Global Trade Item Number
          Catalogue Number GTIN
          420099-1MGCN 04055977187878
          420099-500UGCN 04055977187885

          Documentation

          JAK Inhibitor I - CAS 457081-03-7 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          JAK Inhibitor I - CAS 457081-03-7 - Calbiochem 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.

          Brochure

          Title
          An Introduction to Inhibitors and Their Biological Applications - 1st Edition
          Pathways and Biomarkers of JAK/STAT Signaling

          Technical Info

          Title
          JAK/STAT Signaling Research Focus

          Data Sheet

          Title
          Reprogramming Cell Fate and Function Novel Strategies for iPSC Generation, Characterization, and Differentiation

          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 formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (5 mg/ml)
          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
          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.
          		•