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530153 JAK2 Inhibitor X, FLLL32 - Calbiochem

530153
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₈H₃₂O₆

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      Glass bottle 25 mg
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      Description
      OverviewA cell permeable diketone analog of curcumin that acts as a specific inhibitor of JAK2 (~ 5 µM) and blocks STAT3 phosphorylation in MDA-MB-231 breast and PANC-1 pancreatic cancer cells. However, it does not affect STAT3 phosphorylation in normal human mammary epithelial cells or human pancreatic duct epithelial cells. Does not block the activity of tyrosine kinases containing SH2 and SH2-SH3 domains and several other kinases, such as Akt2, Cdk2-cyclin D1, EGFR kinase, Met, and EbrB2/Her2 kinase (IC50 > 100 µM). Also shown to block DNA binding activity of STAT3. Significantly reduces the viability and invasion capacity of various cancer cells (IC50 = 640 nM; 110 nM, 140 nM, 600 nM, 400 nM in PANC-1, HPAC, MDA-MB-231, SK-BR3, and SUM-159 cells, respectively) and induces apoptosis. Shown to significantly reduce tumor burdens in the MDA-MB-231 xenografted mice.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number530153
      Brand Family Calbiochem®
      SynonymsSTAT3 Signaling Inhibitor, FLLL32
      References
      ReferencesWu, J., et al. 2014. Oncogene 33,173.
      Onimoe, G., et al. 2012. Invest. New Drugs 30, 916.
      Li, L., et al. 2010. Cancer Res. 70, 2445.
      Product Information
      FormYellow powder
      Hill FormulaC₂₈H₃₂O₆
      Chemical formulaC₂₈H₃₂O₆
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetJAK2
      Primary Target IC<sub>50</sub>5 µ
      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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      JAK2 Inhibitor X, FLLL32 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Wu, J., et al. 2014. Oncogene 33,173.
      Onimoe, G., et al. 2012. Invest. New Drugs 30, 916.
      Li, L., et al. 2010. Cancer Res. 70, 2445.
      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.

      Revision28-April-2014 JSW
      SynonymsSTAT3 Signaling Inhibitor, FLLL32
      DescriptionA cell permeable diketone analog of curcumin that acts as a specific inhibitor of JAK2 (~ 5 µM) and blocks STAT3 phosphorylation in MDA-MB-231 breast and PANC-1 pancreatic cancer cells. However, it does not affect STAT3 phosphorylation in normal human mammary epithelial cells or human pancreatic duct epithelial cells. Does not block the activity of tyrosine kinases containing SH2 and SH2-SH3 domains and several other kinases, such as Akt2, Cdk2-cyclin D1, EGFR kinase, Met, and EbrB2/Her2 kinase (IC50 > 100 µM). Also shown to block DNA binding activity of STAT3. Significantly reduces the viability and invasion capacity of various cancer cells (IC50 = 640 nM; 110 nM, 140 nM, 600 nM, 400 nM in PANC-1, HPAC, MDA-MB-231, SK-BR3, and SUM-159 cells, respectively) and induces apoptosis. Shown to significantly reduce tumor burdens in the MDA-MB-231 xenografted mice.
      FormYellow powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₈H₃₂O₆
      Purity≥98% by HPLC
      SolubilityDMSO (100 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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesWu, J., et al. 2014. Oncogene 33,173.
      Onimoe, G., et al. 2012. Invest. New Drugs 30, 916.
      Li, L., et al. 2010. Cancer Res. 70, 2445.