| Identification | Back Directory | [Name]
Supinoxin | [CAS]
888478-45-3 | [Synonyms]
RX-5902
Supinoxin
Supinoxin (RX-5902)
RX-5902 (SUPINOXIN)
4-(3,5-dimethoxyphenyl)-N-(7-fluoro-3-methoxyquinoxalin-2-yl)piperazine-1-carboxamide
1-(3,5-dimethoxyphenyl)-4-[(6-fluoro-2-methoxyquinoxalin-3-yl)aminocarbonyl]piperazine
1-Piperazinecarboxamide, 4-(3,5-dimethoxyphenyl)-N-(7-fluoro-3-methoxy-2-quinoxalinyl)-
breast,inhibit,PANC-1,Inhibitor,Supinoxin,HCT116,UMRC2,PC-3,MKN-45,TNBC,HepG2,DNA/RNA Synthesis,RNA helicase,HT29,cancer,Apoptosis,A549,Caki-1,RX5902,RX 5902 | [Molecular Formula]
C22H24FN5O4 | [MDL Number]
MFCD32004516 | [MOL File]
888478-45-3.mol | [Molecular Weight]
441.46 |
| Hazard Information | Back Directory | [Uses]
Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM[1][2]. | [in vivo]
RX-5902 (oral administration; 160/320/600 mg/kg; once weekly for 3 weeks) significant dose-dependent tumor growth inhibition (TGI) in the MDA-MB-231 model, exhibits TGI of 55.7%, 80.29% and 94.58% at 160 mg/kg, 320 mg/kg and 600 mg/kg, respectively. It is more efficacious than the chemotherapy control arm of nab-paclitaxel (TGI 45%)[1]. | Animal Model: | MDAMD-231 xenograft model in mice[1] | | Dosage: | 160 mg/kg; 320 mg/kg; 600 mg/kg | | Administration: | Oral administration; once weekly for 3 weeks | | Result: | Decreased tumor volume as a dose-dependent manner. |
| [References]
[1] Kost GC, et al. A Novel Anti-Cancer Agent, 1-(3,5-Dimethoxyphenyl)-4-[(6-Fluoro-2-Methoxyquinoxalin-3-yl)Aminocarbonyl] Piperazine (RX-5902), Interferes With β-Catenin Function Through Y593 Phospho-p68 RNA Helicase.J Cell Biochem.?2015 Aug;116(8):1595-601. DOI:10.1002/jcb.25113
[2] Capasso A, et al. First-in-Class Phosphorylated-p68 Inhibitor RX-5902 Inhibits β-Catenin Signaling and Demonstrates Antitumor Activity in Triple-Negative Breast Cancer.Nov;18(11):1916-1925. DOI:10.1158/1535-7163.MCT-18-1334 |
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