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CX-5461

Chemical Structure : CX-5461

CAS No.: 1138549-36-6

CX-5461 (Pidnarulex;CX5461)

Catalog No.: PC-43493Not For Human Use, Lab Use Only.

Pidnarulex (CX-5461) is the first potent, selective, orally bioavailable inhibitor of RNA polymerase I, selectively inhibits rRNA synthesis in HCT-116 cells with IC50 of 142 nM, 200-fold selectivity over Pol II.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Pidnarulex (CX-5461) is the first potent, selective, orally bioavailable inhibitor of RNA polymerase I, selectively inhibits rRNA synthesis in HCT-116 cells with IC50 of 142 nM, 200-fold selectivity over Pol II.
Pidnarulex (CX-5461) inhibits the initiation stage of rRNA synthesis and induces both senescence and autophagy, but not apoptosis, through a p53-independent process in solid tumor cell lines.
Pidnarulex (CX-5461) demonstrates in vivo antitumor activity against human solid tumors in murine xenograft models.

Physicochemical Properties

M.Wt
Formula C27H27N7O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: < 5.3 mg/mL

Chemical Name/SMILES

5H-Benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide, 2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-N-[(5-methyl-2-pyrazinyl)methyl]-5-oxo-

References

1. Haddach M, et al. ACS Med Chem Lett. 2012 May 8;3(7):602-6.

2. Drygin D, et al. Cancer Res. 2011 Feb 15;71(4):1418-30.

3. Bywater MJ, et al. Cancer Cell. 2012 Jul 10;22(1):51-65.

4. Achiron A, et al. J Neuroimmunol. 2013 Oct 15;263(1-2):91-7.

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