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

A cell-permeable, selective inhibitor of RNA polymerase I-mediated pre-rRNA transcription (IC₅₀ = 142 nM in HCT-116 cells).

RNA Polymerase I Inhibitor II, CX-5461 - CAS 1138549-36-6 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Pol I Inhibitor II, CX5461, 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

Primary Target: Pol I multi-protein complex
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509265
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1138549-36-6C₂₇H₂₇N₇O₂S

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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®
      SynonymsPol I Inhibitor II, CX5461, 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
      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
      Quality LevelMQ100
      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
      Global Trade Item Number
      Catalogue Number GTIN
      5.09265.0001 04055977241730

      Documentation

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

      Title

      Safety Data Sheet (SDS) 

      RNA Polymerase I Inhibitor II, CX-5461 - CAS 1138549-36-6 - Calbiochem Certificates of Analysis

      TitleLot Number
      509265

      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
      SynonymsPol I Inhibitor II, CX5461, 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
      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 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
      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.