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CX-5461Pol I-mediated rRNA synthesis inhibitor

CX-5461

Catalog No. A8337
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $110.00 In stock
10mg $170.00 In stock
50mg $540.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Rossetti S, Wierzbicki AJ, Sacchi N. "Mammary epithelial morphogenesis and early breast cancer. Evidence of involvement of basal components of the RNA Polymerase I transcription machinery." Cell Cycle. 2016 Aug 2:0. PMID:27485818

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Chemical structure

CX-5461

Related Biological Data

CX-5461

Related Biological Data

CX-5461

Biological Activity

Description CX-5461 is an inhibitor of rRNA synthesis with IC50 of 142 nM for Pol I-driven transcription of rRNA,
Targets Pol I HCT-116 A375 MIA PaCa-2    
IC50 142 nM 167 nM (ED50) 58 nM (ED50) 74 nM (ED50)    

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Chemical Properties

Cas No. 1138549-36-6 SDF Download SDF
Synonyms CX 5461;CX5461
Chemical Name 2-(4-methyl-1,4-diazepan-1-yl)-N-[(5-methylpyrazin-2-yl)methyl]-5-oxo-[1,3]benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide
Canonical SMILES CC1=CN=C(C=N1)CNC(=O)C2=C3N(C4=CC=CC=C4S3)C5=C(C2=O)C=CC(=N5)N6CCCN(CC6)C
Formula C27H27N7O2S M.Wt 513.61
Solubility Limited solubility Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

CX-5461 is a potent and orally bioavailable small-molecule inhibitor of rRNA synthesis that specifically inhibits RNA polymerase (Pol) I-driven transcription with IC50 value of 142 nM. CX-5461 exhibits antiproliferative activity against human pancreatic tumor cells MIA Paca-2, human melanoma cells A375 and colorectal carcinoma cells HCT-116 with EC50 values of 74, 58, and 167 nmol/L, respectively. [1].

CX-5461 was revealed to inhibit Pol I transcription via promoting the stabilization of p53. In addition, CX-5461 has been demonstrated to induce autophagy and senescence but not apoptosis in MIA Paca-2 and A375 cell lines.

In vivo, CX-5461 has shown to suppress tumor volume in both MIA Paca-2 and A375 derived xenograft mice models [1].

References:
[1] Drygin D1, Lin A, Bliesath J, Ho CB, O'Brien SE, Proffitt C, Omori M, Haddach M, Schwaebe MK, Siddiqui-Jain A, Streiner N, Quin JE, Sanij E, Bywater MJ,Hannan RD, Ryckman D, Anderes K, Rice WG. Targeting RNA polymerase I with an oral small molecule CX-5461 inhibits ribosomal RNA synthesis and solid tumor growth. Cancer Res. 2011 Feb 15;71(4):1418-30