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509265 Sigma-AldrichRNA 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.

MSDS
分析证书
参考
Data Sheet

同义词: 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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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
1138549-36-6	C₂₇H₂₇N₇O₂S

价格及供货情况

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Description
Overview	A 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 Number	509265
Brand Family	Calbiochem®
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

References
References	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.

Product Information
CAS number	1138549-36-6
Form	Light beige powder
Hill Formula	C₂₇H₂₇N₇O₂S
Chemical formula	C₂₇H₂₇N₇O₂S
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	Pol I multi-protein complex
Purity	≥97% by HPLC

Physicochemical Information
Cell permeable	Y

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 Instructions	Following 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
产品目录编号	GTIN
5.09265.0001	04055977241730

Documentation

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

职位
物料安全数据表 (MSDS)

RNA Polymerase I Inhibitor II, CX-5461 - CAS 1138549-36-6 - Calbiochem 分析证书

标题	批号
509265	输入批号

参考

参考信息概述
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.

数据表

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.

Revision	21-February-2014 JSW
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
Description	A 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.
Form	Light beige powder
Intert gas (Yes/No)	Packaged under inert gas
CAS number	1138549-36-6
Chemical formula	C₂₇H₂₇N₇O₂S
Structure formula
Purity	≥97% by HPLC
Solubility	DMSO (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 Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity	Standard Handling
References	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.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Other Inhibitors of Biological Interest

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