|CX-5461Pol I-mediated rRNA synthesis inhibitor|
Sample solution is provided at 25 µL, 10mM.
|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)|
|Cas No.||1138549-36-6||SDF||Download SDF|
|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
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. .
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 .
 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