CX-5461 | B2183

CX-5461 is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC₅₀s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC₅₀ ≥25 μM). At 50 mg/kg, CX-5461 demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.

CX-5461 is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC₅₀s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC₅₀ ≥25 μM). At 50 mg/kg, CX-5461 demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.

B2183 | CX-5461 DataSheet

Alternate Name/Synonyms: 2-(4-methyl-1,4-diazepan-1-yl)-N-((5-methylpyrazin-2-yl)methyl)-5-oxo-5H-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxamide

Appearance: Crystalline solid

Formulation: N/A

CAS Number: 1138549-36-6

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₇H₂₇N₇O₂S

Molecular Weight: 513.61

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis

MDL Number: N/A

PubChem CID: 25257557

SMILES: CC1=CN=C(C=N1)CNC(=O)C2=C3N(C4=CC=CC=C4S3)C5=C(C2=O)C=CC(=N5)N6CCCN(CC6)C

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)

InChi Key: XGPBJCHFROADCK-UHFFFAOYSA-N