RA-9 |
カタログ番号GC60317
One-Click Copy Product Info
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RA-9 は、強力で選択的なプロテアソーム関連脱ユビキチン化酵素 (DUB) 阻害剤であり、好ましい毒性プロファイルと抗がん活性を備えています。 RA-9 は、20S プロテアソームのタンパク質分解活性に影響を与えることなく、ユビキチン依存性タンパク質の分解をブロックします。 RA-9 は、卵巣癌細胞株およびドナー由来の初代培養において、アポトーシスの開始を選択的に誘導します。 RA-9 は、卵巣癌細胞で小胞体 (ER) ストレス応答を誘導します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 919091-63-7
Sample solution is provided at 25 µL, 10mM.
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RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells[1].
RA-9 (10-30 μM; 48 hours) inhibits growth of ovarian cancer cell lines and primary cultures[1].RA-9 (1.25-5 μM; 18 hours) causes cell cycle arrest and caspase-mediated apoptosis in ovarian cancer cells[1].RA-9 (5 μM; 0-24 hours) induces ER-stress responses in ovarian cancer cells[1].RA-9 (5 μM; over 24 hours) treatment results with time-dependent accumulation of the cleaved formed of PARP noticeable as early as 8 hours[1]. Cell Viability Assay[1] 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
RA-9 (5 mg/kg; i.p; one-day on, two-days off) inhibits human ovarian cancer cell growth in vivo and prolongs survival in a mouse model for ovarian cancer[1]. Animal Model: Six-week-old female immunodeficient (NCr nu/nu) mice[1]
[1]. Coughlin K, 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.
| Cas No. | 919091-63-7 | SDF | |
| Canonical SMILES | O=C1/C(CNC/C1=C\C2=CC=C([N+]([O-])=O)C=C2)=C/C3=CC=C([N+]([O-])=O)C=C3 | ||
| Formula | C19H15N3O5 | M.Wt | 365.34 |
| 溶解度 | DMSO: 4.17 mg/mL (11.41 mM; ultrasonic and warming and heat to 80°C) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7372 mL | 13.6859 mL | 27.3718 mL |
| 5 mM | 547.4 μL | 2.7372 mL | 5.4744 mL |
| 10 mM | 273.7 μL | 1.3686 mL | 2.7372 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)