CX-5461, Inhibitor

CX-5461

Cat. Num. AAA3600488

• Purity: >98% (HPLC)
• Synonyms: CX-5461; CX 5461; CX5461; inhibitor

• Purity/Purification: >98% (HPLC)

• Suitability: DMSO: <5.3mg/mL
• Target: DNA/RNA Synthesis
• Receptor: PolI-driventranscriptionofrRNA
• Chemical Name: 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
• SMILES: O=C(C1=C(SC2=CC=CC=C23)N3C4=C(C=CC(N5CCN(C)CCC5)=N4)C1=O)NCC6=NC=C(C)N=C6
• Molecular Formula: C27H27N7O2S
• CAS Number: 1138549-36-6
• Preparation and Storage: Store at -20 degree C; Stability: >=2 years; Shipping: Ice Pack

Structure

Related Product Information for CX-5461, inhibitor

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 142nM, 200-fold selectivity over Pol II; 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; demonstrates in vivo antitumor activity against human solid tumors in murine xenograft models. Solid Tumors Phase 2 Clinical

Product Categories/Family for CX-5461, inhibitor

Solid Tumors; Cell Cycle/DNA Damage; Cancer

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.