509265 RNA Polymerase I Inhibitor II, CX-5461 - CAS 1138549-36-6 - Calbiochem

509265
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₇H₂₇N₇O₂S 1138549-36-6

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.09265.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable benzothiazole compound that selectively inhibits RNA polymerase I-mediated pre-rRNA transcription (IC50 = 142 nM in HCT-116), but not Pol II-mediated c-myc transcription, by preventing TAF SL1 and rDNA association). Effectively inhibits Pol I-dependent proliferation among 39 cancer cell lines (IC50 <1 µM) in vitro and suppresses A375 (50 mg/kg/d p.o.) and MIA PaCa-2 (50 mg/kg/3d p.o.) tumor expansion in vivo.
          Catalogue Number509265
          Brand Family Calbiochem®
          SynonymsCX5461, 2-(4-Methyl-1,4-diazepan-1-yl)-N-((5-methylpyrazin-2-yl)methyl)-5-oxo-5H-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxamide, Pol I Inhibitor II
          References
          ReferencesHaddach, M., et al. 2012. ACS Med. Chem. Lett. 3, 602.
          Bywater, M.J., et al. 2012. Cancer Cell 22, 51.
          Drygin, D., et al. 2011. Cancer Res 71, 1418.
          Product Information
          CAS number1138549-36-6
          FormLight beige powder
          Hill FormulaC₂₇H₂₇N₇O₂S
          Chemical formulaC₂₇H₂₇N₇O₂S
          ReversibleY
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary TargetPol I multi-protein complex
          Purity≥97% 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
          Haddach, M., et al. 2012. ACS Med. Chem. Lett. 3, 602.
          Bywater, M.J., et al. 2012. Cancer Cell 22, 51.
          Drygin, D., et al. 2011. Cancer Res 71, 1418.
          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.

          Revision21-February-2014 JSW
          SynonymsCX5461, 2-(4-Methyl-1,4-diazepan-1-yl)-N-((5-methylpyrazin-2-yl)methyl)-5-oxo-5H-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxamide, Pol I Inhibitor II
          DescriptionA cell-permeable benzothiazole compound that selectively inhibits RNA polymerase I-mediated pre-rRNA transcription (IC50 = 142, 113, 54, and 74 nM in HCT-116, A375, MIA PaCa-2, and BJ-hTert cells, respectively), but not Pol II-mediated c-myc transcription, by preventing TAF (TATA Binding Protein-/TBP-Associated Factor) SL1 and rDNA association, effectively inhibiting Pol I-dependent proliferation among 39 cancer cell lines (IC50 <1 µM) in vitro. While Pol I inhibition by CX-5461 is shown to result in p53-dependent apoptosis in cancer cells of hematopoietic origin, cell death by CX-5461 treatment in solid tumors-derived A375 and MIA PaCa-2 cultures are primarily due to autophagy and senescence, but not apoptosis, induction. Shown to suppress A375 (50 mg/kg/d p.o.) and MIA PaCa-2 (50 mg/kg/3d p.o.) tumor expansion, as well as selectively induce p53-mediated cell death of Eμ-Myc lymphoma, but not normal B cells, in mice (50 mg/kg p.o.) in vivo.
          FormLight beige powder
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1138549-36-6
          Chemical formulaC₂₇H₂₇N₇O₂S
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (0.5 mg/ml) or Dilute Acetic Acid (10 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
          ReferencesHaddach, M., et al. 2012. ACS Med. Chem. Lett. 3, 602.
          Bywater, M.J., et al. 2012. Cancer Cell 22, 51.
          Drygin, D., et al. 2011. Cancer Res 71, 1418.