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420151 JAK2 Inhibitor IX, WP1193

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420151
  
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      Overview

      Replacement Information
      Description
      Overview

      This product has been discontinued.



      A cell-permeable tyrphostin WP1130 (Cat. No. 681685) analog that inhibits JAK2 kinase activity (by >90% at 2.5 µM in in vitro kinase assays) and effectively suppresses JAK2-dependent STAT3 Tyr705 phosphorylation in murine melanoma B16 and human GSC (glioma stem-like cell) cultures (5 µM), as well as JAK2-dependent Bcr-Abl Tyr177 phosphorylation in primary human CML PBMCs, Imatinib/STI571-sensitive 32DP210, and IM-resistant Ba/F3-T315I murine leukemia lines (10 µM). Reported to inhibit the growths of IM-resistant K562-R and T315I+ 32D in murine leukemia models (30 mg/kg via i.p.; q.o.d.), as well as synergize with INF-α in suppressing B16 blood-to-lung metastasis and eliminating LMD (lentiginous melanocytic dysplasia) in mice died from established B26-derived brain tumor (30 mg WP1130/kg via o.g./oral gavage) in vivo.

      Catalogue Number420151
      Brand Family Calbiochem®
      Synonyms(S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(cyclopropyl(phenyl)methyl)acrylamide
      References
      ReferencesSai, K., et al. 2012. J. Neurooncol. 107, 487.
      Samanta, A., et al. 2011. Leukemia 25, 463.
      Kong, L.Y., et al. 2010. Clin. Cancer Res. 16, 2550.
      Product Information
      FormBrown solid
      Hill FormulaC₁₉H₁₆BrN₃O
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetJAK2
      Purity≥95% 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 +2°C to +8°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 6 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
      420151 0

      Documentation

      JAK2 Inhibitor IX, WP1193 SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Sai, K., et al. 2012. J. Neurooncol. 107, 487.
      Samanta, A., et al. 2011. Leukemia 25, 463.
      Kong, L.Y., et al. 2010. Clin. Cancer Res. 16, 2550.

      Technical Info

      Title
      JAK/STAT Signaling Research Focus
      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.

      Revision23-August-2012 JSW
      Synonyms(S,E)-3-(6-Bromopyridin-2-yl)-2-cyano-N-(cyclopropyl(phenyl)methyl)acrylamide
      DescriptionA cell-permeable tyrphostin WP1130 (Cat. No. 681685) analog that inhibits JAK2 kinase activity (by >90% at 2.5 µM in in vitro kinase assays) and effectively suppresses JAK2-dependent STAT3 Tyr705 phosphorylation in murine melanoma B16 and human GSC (glioma stem-like cell) cultures (5 µM), as well as JAK2-dependent Bcr-Abl Tyr177 phosphorylation in primary human CML PBMCs, Imatinib/STI571-sensitive 32DP210, and IM-resistant Ba/F3-T315I murine leukemia lines (10 µM). Reported to inhibit the growths of IM-resistant K562-R and T315I+ 32D in murine leukemia models (30 mg/kg via i.p.; q.o.d.), as well as synergize with INF-α in suppressing B16 blood-to-lung metastasis and eliminating LMD (lentiginous melanocytic dysplasia) in mice died from established B26-derived brain tumor (30 mg WP1130/kg via o.g./oral gavage) in vivo.
      FormBrown solid
      Intert gas (Yes/No) Packaged under inert gas
      Purity≥95% by HPLC
      SolubilityMethanol (1 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesSai, K., et al. 2012. J. Neurooncol. 107, 487.
      Samanta, A., et al. 2011. Leukemia 25, 463.
      Kong, L.Y., et al. 2010. Clin. Cancer Res. 16, 2550.