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

420099
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概要

Replacement Information

主要スペック表

Empirical Formula
C₁₈H₁₆FN₃O

価格&在庫状況

カタログ番号 在庫状況包装 Qty/Pk 価格 数量
420099-1MGCN
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      樹脂アンプル 1 mg
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      420099-500UGCN
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          樹脂アンプル 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, DBI, Pyridone 6, P6, 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

          Documentation

          JAK Inhibitor I - CAS 457081-03-7 - Calbiochem (M)SDS

          タイトル

          英語版製品安全データシート((M)SDS) 

          JAK Inhibitor I - CAS 457081-03-7 - Calbiochem 試験成績書(CoA)

          タイトルロット番号
          420099

          参考資料

          参考資料の概要
          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.

          カタログ

          タイトル
          Pathways and Biomarkers of JAK/STAT Signaling

          技術情報

          タイトル
          JAK/STAT Signaling Research Focus

          引用

          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.
        • データシート

          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.