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产品名称 CX 5461
产品货号 Axon 2173 CAS [1138549-36-6] MF C27H27N7O2SMW 513.61 Purity: 99% Soluble in 0.1N HCl(aq) Description First selective inhibitor of RNA Polymerase I (Pol I or RNAP1, IC50 of 0.88 μM) transcription with in vivo activity in tumor growth efficacy models; potent and orally bioavailable. CX 5461 demonstrated approximately 200-fold selectivity against Pol I relative to Pol II. It selectively kills tumor cells by activating p53-dependent apoptosis. It also shows potent antiproliferative capacity in human hematologic tumor cells. References Certificates Categories Extra info M. Haddach et al. Discovery of CX-5461, the first direct and selective inhibitor of RNA Polymerase I, for cancer therapeutics. ACS Med. Chem. Lett. 2012, 3, 602-606.   M.J. Bywater et al. Inhibition of RNA polymerase I as a therapeutic strategy to promote cancer-specific activation of p53. Cancer Cell 2012, 22, 51-65. Certificate of Analysis Material Safety Data Sheet Cell Cycle Regulation Cell Signaling & Oncology Immunology RNAP1 p53-Tumor Suppression DNA-damage Response EC 2.7.7.6 Inhibitor of RNA Polymerase I (RNAP1) Chemical name 2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-N-[(5-methyl-2-pyrazinyl)methyl]-5-oxo-5H-Benzothiazolo[3,2-a][1,8]naphthyridine-6-carboxamide Parent CAS No. [1138549-36-6] Order Size Unit Price Stock 5 mg €135.00 In Stock
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CX 5461

Based on 8 reference(s) in Google Scholar 9 10 8

Axon 2173

CAS [1138549-36-6]

MF C27H27N7O2S
MW 513.61

  • Purity: 99%
  • Soluble in 0.1N HCl(aq)

CX 5461

Description

First selective inhibitor of RNA Polymerase I (Pol I or RNAP1, IC50 of 0.88 μM) transcription with in vivo activity in tumor growth efficacy models; potent and orally bioavailable. CX 5461 demonstrated approximately 200-fold selectivity against Pol I relative to Pol II. It selectively kills tumor cells by activating p53-dependent apoptosis. It also shows potent antiproliferative capacity in human hematologic tumor cells.
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