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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

Pricing & Availability

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420099-500UG
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      		 Plastic ampoule 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 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
      420099-500UG 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.
      		•