RA-9
(3E,5E)-3,5-Bis[(4-nitrophenyl)methylene]-4-piperidinone
CAS: 919091-63-7
Molecular Formula: C19H15N3O5
RA-9 - Names and Identifiers
RA-9 - Physico-chemical Properties
| Molecular Formula | C19H15N3O5 |
| Molar Mass | 365.34 |
| Density | 1.414±0.06 g/cm3(Predicted) |
| Melting Point | 230-233 °C(Solv: ethyl ether (60-29-7); acetonitrile (75-05-8)) |
| Boling Point | 588.5±50.0 °C(Predicted) |
| Solubility | DMSO: 2 mg/mL , ultrasonic and warming and heat to 80°C mother liquor preservation: sub-packaging and freezing to avoid repeated freezing and thawing;-20 ℃,1 month;-80 ℃,6 months (after dilution, the solution temperature is low and storage may precipitate, as far as possible to use the current preparation) cell experiment: dissolve with DMSO first, dilute with culture medium, and the dilution process is recommended to be carried out in sections, avoid too fast concentration change causing compound precipitation. If the compound is precipitated during the dilution process, it can be redissolved by ultrasound. During dilution, ensure that the final concentration of DMSO in the working fluid should be below 0.1% as far as possible, and the maximum should not exceed 0.5%, and set up a DMSO control group with corresponding concentration. Animal experiment: Dissolve with DMSO first: dilute with water or normal saline, etc. The dilution process is recommended to be carried out in sections to |
| pKa | 5.13±0.20(Predicted) |
| Storage Condition | -20℃ |
| Use | RA-9 is a cell permeable and potent inhibitor of the ubiquitin-proteasome system (UPS). RA-9 Inhibits Proteasome-Associated DUBs and Ovarian Cancer in Vitro and in Vivo via Exacerbating Unfolded Protein Responses. Treatment with RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. Loss of cell viability following RA-9 exposure is associated with an unfolded protein response as mechanism to compensate for unsustainable levels of proteotoxic stress. In vivo treatment with RA-9 retards tumor growth, increases overall survival, and was well tolerated by the host. |
RA-9 - Reference
| Reference Show more | 1. Coughlin K, Anchoori R, Iizuka Y, et al. Small-molecule RA-9 inhibits proteasome-associated DUBs and ovarian cancer in vitro and in vivo via exacerbating unfolded protein responses. Clin Cancer Res. 2014;20(12):3174‐3186. doi:10.1158/1078-0432.CCR-13-2658 |
RA-9 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.739 ml | 13.695 ml | 27.39 ml |
| 5 mM | 0.548 ml | 2.739 ml | 5.478 ml |
| 10 mM | 0.274 ml | 1.369 ml | 2.739 ml |
| 5 mM | 0.055 ml | 0.274 ml | 0.548 ml |
Last Update：2024-01-02 23:10:35
RA-9 - Animal Experiment
Mice were inoculated i.p. with 100,000 ES-2 cells (in 100 μl DMEM) stably expressing GFP. When tumor was detectable (approx. 6 days post inoculation), mice were randomly assigned into two groups receiving RA-9 or 0.9% saline. Treatment with RA-9 was given i.p. on a one-day on, two-days off schedule. The control group received the vehicle alone at the same schedule. Working concentrations of RA-9 (10 mg/ml) were reached by dissolution in Cremophor EL and polyethylene glycol 400 (Sigma). Prior to each injection RA-9 was further diluted in 0.9% saline (working concentration 1mg/ml). To monitor for tumor growth, RA-9 treated and control mice were imaged with an IVIS SpectrumCT Pre-clinical in vivo imaging system (PerkinElmer) every other day. Animals were sacrificed when abdomens became distended to twice normal size.
Last Update：2023-08-16 21:32:38
RA-9 - Reference Information
| biological activity | RA-9 is a cell-permeable proteasome-associated deubiquinting enzymes (DUBs) potent Selective inhibitors, with good toxicity and anticancer activity. RA-9 can selectively induce apoptosis in ovarian cancer cell lines. |
| Target | Value |
| Cell Line: | Cisplatin-sensitive ovarian cancer cell lines TOV-21G and ES-2, Cisplatin-resistant ovarian cancer cell lines HEY and OVCAR-3, primary ovarian cancer cells ES-2 cells ES-2, SKOV-3 and TOV-21G ovarian cancer cells |
| Concentration: | 10, 20, 30 μM 1.25, 5 μM 5 μM |
| Incubation Time: | 48 hours 18 hours 0-24 h |
| Result: | Compromised the viability of ovarian cancer cells in a dose-dependent fashion. Resulted in a dose-dependent increase in the fraction of ES-2 cells in the G2-M cell cycle phase. Caused a time-dependent increase in the steady levels of the early ER-stress marker GRP-78, as well as the late ER-stress markers IRE1-α and Ero1L-α. Significant reduction in tumor burden at day 12. |
| Animal Model: | Six-week-old female immunodeficient (NCr nu/nu) mice |
| Dosage: | 5 mg/kg |
| Administration: | I.p; one-day on, two-days off |
Last Update：2024-04-09 20:52:54
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Spot supply
Product Name: (3E,5E)-3,5-Bis[(4-nitrophenyl)methylene]-4-piperidinone Visit Supplier Webpage Request for quotationCAS: 919091-63-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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