420151 | JAK2 Inhibitor IX, WP1193

420151
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      420151-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA 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
          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

          Documentation

          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 +2°C to +8°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 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.