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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 $132.00 In stock
10mg $220.00 In stock
50mg $616.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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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