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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
420099
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
457081-03-7C₁₈H₁₆FN₃O

Products

Catalogue NumberPackaging Qty/Pack
420099-1MG Plastic ampoule 1 mg
420099-500UG Plastic ampoule 500 μg
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
420099-1MG 04055977187878
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.
    		•