| Chemical Properties | Back Directory | [Boiling point ]
857.537±65.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.428±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
12.718±0.46(predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
RA375 is a RPN13 (26S proteasome regulatory subunit) inhibitor. RA375 activates UPR signaling, ROS production and apoptosis. RA375 exhibits ten-fold greater activity against cancer lines than RA190, reflecting its nitro ring substituents and the addition of a chloroacetamide warhead[1]. | [in vivo]
RA375 (10 mg/kg, ip) inhibits proteasome function and reduces ovarian tumor burden in mice[1]. | Animal Model: | RA375 (10 mg/kg, ip) inhibits proteasome function and reduces ovarian tumor burden in mice[1]. | | Dosage: | 10 mg/kg. | | Administration: | IP for a 5 days on, 2 days off cycle for two weeks. | | Result: | Reduced ovarian tumor burden in mice. |
| Animal Model: | Female Balb/c mice[1]. | | Dosage: | 5, 10, 20, 40, 60, 100 mg/kg (Pharmacological Analysis). | | Administration: | IP single dose. | | Result: | The dose of 40 mg/kg on alternate days for two weeks produced no observable toxicities or weight loss. |
| [References]
[1] Ravi K Anchoori, et al. Structure-function Analyses of Candidate Small Molecule RPN13 Inhibitors With Antitumor Properties. PLoS One. 2020 Jan 15;15(1):e0227727. DOI:10.1371/journal.pone.0227727 |
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