| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
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.
| ln Vitro |
The growth of primary cultures and cell lines of ovarian cancer is inhibited by RA-9 (10-30 μM; 48 hours) [1].
In ovarian cancer cells, RA-9 (1.25-5 μM; 18 hours) induces cell cycle arrest and caspase-mediated apoptosis [1].
Inducing ER-stress responses in ovarian cancer cells, RA-9 (5 μM; 0-24 hours) [1].
RA-9 (5 μM; more than a day) treatment outcomes, with as early as eight hours of time-dependent accumulation of the cleaved form of PARP [1].
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| ln Vivo |
In a mouse model of ovarian cancer, RA-9 (5 mg/kg; i.p.; one day on, two days off) prolongs survival by inhibiting the growth of human ovarian cancer cells in vivo [1].
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| Animal Protocol |
Six-week-old female immunodeficient (NCr nu/nu) mice [1].
5 mg/kg |
| References |
| Molecular Formula |
C19H15N3O5
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|---|---|
| Molecular Weight |
365.345
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| Exact Mass |
365.101
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| Elemental Analysis |
C, 62.46; H, 4.14; N, 11.50; O, 21.90
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| CAS # |
919091-63-7
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| Related CAS # |
919091-63-7
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| PubChem CID |
5469266
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.517
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
27
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| Complexity |
591
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(/C1C=CC([N+](=O)[O-])=CC=1)=C1/CNC/C(=C\C2C=CC([N+](=O)[O-])=CC=2)/C/1=O
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| InChi Key |
YUYPWAMLWZVHAE-KAVGSWPWSA-N
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| InChi Code |
InChI=1S/C19H15N3O5/c23-19-15(9-13-1-5-17(6-2-13)21(24)25)11-20-12-16(19)10-14-3-7-18(8-4-14)22(26)27/h1-10,20H,11-12H2/b15-9+,16-10+
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| Chemical Name |
(3E,5E)-3,5-Bis[(4-nitrophenyl)methylene]-4-piperidinone
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| Synonyms |
RA-9; RA 9; RA9; RA-9 UPS inhibitor
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :4.17~8 mg/mL ( 11.41~21.89 mM )
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7371 mL | 13.6855 mL | 27.3710 mL | |
| 5 mM | 0.5474 mL | 2.7371 mL | 5.4742 mL | |
| 10 mM | 0.2737 mL | 1.3686 mL | 2.7371 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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