CX-5461

CX-5461 is an inhibitor of ribosomal RNA (rRNA) synthesis. It selectively inhibits RNA polymerase I-driven transcription of rRNA in HCT116, A375, and MIA PaCa-2 tumor cells (IC50s = 142, 113, and 54 nM, respectively) without affecting RNA polymerase II (IC50 > 25µM), DNA replication, or protein translation. At 50 mg/kg, CX-5461 demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.Formal 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. CAS Number: 1138549-36-6. Molecular Formula: C27H27N7O2S. Formula Weight: 513.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 1 mg/ml, Ethanol: 0.1 mg/ml. lambdamax: 242, 292, 299, 339 nm. SMILES: CC1=NC=C(CNC(C2=C3N(C(C=CC=C4)=C4S3)C5=C(C=CC(N6CCCN(C)CC6)=N5)C2=O)=O)N=C1. InChi Code: 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). InChi Key: XGPBJCHFROADCK-UHFFFAOYSA-N.