506387 | gp130 Inhibitor, SC144 - Calbiochem

506387
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₆H11FN₆O·HCl

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.06387.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable, orally active, quinoxalinhydrazide derivative that acts an inhibitor of gp130. Binds to gp130 and induces its phosphorylation at Ser782 in ovarian cancer cells (OVCAR-8 and CaoV-3) in a time and dose-dependent manner. Shown to be cytotoxic in a number of ovarian cancer cell lines (IC50 = 720, 490, 950, 440, 530, 88-0, and 430 nM in OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY, and NCI/ADR-RES cells, respectively). Suppresses constitutive phosphorylation of and nuclear translocation of Stat3. Also blocks LIF and IL-6-induced Akt activation and phosphorylation of Stat3 (Y705) and Stat1 (Y701), without affecting their activation by IFN-γ. Reduces the level downstream effectors of gp130/Stat3 (survivin, MMP-7, Bcl-2, Bcl-xl, and cyclin D1) in ovarian cancer cells. Suppresses the growth of OVCAR-8 tumor xenografts in nude mice without affecting normal tissue (10 mg/kg, i.p. for 58 days).

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number506387
          Brand Family Calbiochem®
          SynonymsSC144
          References
          ReferencesXu, S., et al. 2013. Mol. Cancer Ther. 12, 937.
          Product Information
          FormLight yellow solid
          Hill FormulaC₁₆H11FN₆O·HCl
          Chemical formulaC₁₆H11FN₆O·HCl
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary Targetgp130
          Purity≥98% by HPLC
          Physicochemical Information
          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
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Xu, S., et al. 2013. Mol. Cancer Ther. 12, 937.
          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.

          Revision31-January-2014 JSW
          SynonymsSC144
          DescriptionA cell-permeable, orally active, quinoxalinhydrazide derivative that acts an inhibitor of gp130. Binds to gp130 and induces its phosphorylation at Ser782 in ovarian cancer cells (OVCAR-8 and CaoV-3) in a time and dose-dependent manner. Shown to be cytotoxic in a number of ovarian cancer cell lines (IC50 = 720, 490, 950, 440, 530, 88-0, and 430 nM in OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY, and NCI/ADR-RES cells, respectively). Suppresses constitutive phosphorylation of and nuclear translocation of Stat3. Also blocks LIF and IL-6-induced Akt activation and phosphorylation of Stat3 (Y705) and Stat1 (Y701), without affecting their activation by IFN-γ. Reduces the level downstream effectors of gp130/Stat3 (survivin, MMP-7, Bcl-2, Bcl-xl, and cyclin D1) in ovarian cancer cells. Suppresses the growth of OVCAR-8 tumor xenografts in nude mice without affecting normal tissue (10 mg/kg, i.p. for 58 days).
          FormLight yellow solid
          Chemical formulaC₁₆H11FN₆O·HCl
          Structure formulaStructure formula
          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
          ReferencesXu, S., et al. 2013. Mol. Cancer Ther. 12, 937.