CX-5461, RNA Polymerase I inhibitor

Overview
Catalog #	bs-66052c-2-mg-solid
Product Name	CX-5461, RNA Polymerase I inhibitor
Specifications
Storage Buffer	Powder
Storage Condition	Store in dry, dark place at -20C for 1 year.
Target
Product Information	Molecular Weight: 513.61 Formula: C27 H27 N7 O2 S CAS Number: 1138549-36-6 InChi Key: XGPBJCHFROADCK-UHFFFAOYSA-N InChi: InChI=1S/C27H27N7O2S/c1-17-14-29-18(15-28-17)16-30-26(36)23-24(35)19-8-9-22(33-11-5-10-32(2)12-13-33)31-25(19)34-20-6-3-4-7-21(20)37-27(23)34/h3-4,6-9,14-15H,5,10-13,16H2,1-2H3,(H,30,36) Smiles: CN1CCN(CCC1)C1C=CC2=C(N=1)N1C(SC3=CC=CC=C13)=C(C2=O)C(=O)NCC1C=NC(C)=CN=1 Purity: 98.0 Solubility: DMSO up to 2 mM Appearance: Solid Power. Shelf Life: 1.0 years
Description	CX-5461 is a first-in-class non-genotoxic small molecule targeted inhibitor of RNA polymerase I (Pol I) that activates the p53 pathway without causing DNA damage. CX-5461 selectively inhibits rRNA synthesis by Pol I in the nucleolus, but does not inhibit mRNA synthesis by RNA Polymerase II (Pol II) and does not inhibit DNA replication or protein synthesis. Inhibition of Pol I results in nucleolar stress and release of ribosomal proteins (RP) from the nucleolus. The RP bind to Mdm2 and liberate p53 to orchestrate apoptosis in cancer cells. CX-5461 demonstrates a favorable preclinical profile, potently and selectively kills cancer cells, demonstrates robust in vivo efficacy in multiple models, and has demonstrated oral bioavailability in multiple species.