Product Information
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

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
Pathways and Biomarkers of JAK/STAT Signaling

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, DBI, Pyridone 6, P6, 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 -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.
  • Related Products & Applications

    Categories

    Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > JAK Inhibitors