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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).

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
509265
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1138549-36-6C₂₇H₂₇N₇O₂S

Products

Catalogue NumberPackaging Qty/Pack
5.09265.0001 Glass bottle 10 mg
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 SDS

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.