Pol I-mediated rRNA synthesis inhibitor
CAS：1138549-36-6
分子式：C27H27N7O2S
分子量：513.61
纯度：98%
存储：Store at -20°C

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].

参考文献:
[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