Quarfloxin

Quarfloxin is an inhibitor of RNA polymerase I-mediated transcription. It binds to G-quadruplex DNA and inhibits the interaction between ribosomal DNA G-quadruplexes and nucleolin, a nucleolar protein required for RNA polymerase I-mediated transcription. Quarfloxin (10 µM) induces nucleolin mislocalization from the nucleoli to the nucleoplasm in A549 cells. It induces apoptosis in A549 and HL-60 cells when used at a concentration of 5 µM. Quarfloxin (5 mg/kg) reduces tumor growth in MDA-MB-231 breast and MiaPaCa-2 pancreatic cancer mouse xenograft models.Formal Name: 5-fluoro-N-[2-[(2S)-1-methyl-2-pyrrolidinyl]ethyl]-3-oxo-6-[3-(2-pyrazinyl)-1-pyrrolidinyl]-3H-benzo[b]pyrido[3,2,1-kl]phenoxazine-2-carboxamide. CAS Number: 865311-47-3. Synonyms: CX-3543, Itarnafloxin, Quarfloxacin. Molecular Formula: C35H33FN6O3. Formula Weight: 604.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. lambdamax: 218, 319 nm. SMILES: O=C1C2=C3N(C=C1C(NCC[C@@H]4CCCN4C)=O)C5=CC6=CC=CC=C6C=C5OC3=C(N7CC(C8=NC=CN=C8)CC7)C(F)=C2. InChi Code: InChI=1S/C35H33FN6O3/c1-40-13-4-7-24(40)8-10-39-35(44)26-20-42-29-15-21-5-2-3-6-22(21)16-30(29)45-34-31(42)25(33(26)43)17-27(36)32(34)41-14-9-23(19-41)28-18-37-11-12-38-28/h2-3,5-6,11-12,15-18,20,23-24H,4,7-10,13-14,19H2,1H3,(H,39,44)/t23?,24-/m0/s1. InChi Key: WOQIDNWTQOYDLF-CGAIIQECSA-N.