VR23 |
カタログ番号GC12003
One-Click Copy Product Info
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VR23 は、トリプシン様プロテアソーム (IC50=1 nM)、キモトリプシン様プロテアソーム (IC50=50-100 nM)、およびカスパーゼ様プロテアソーム (IC50=3 μM) の活性を強力に阻害する低分子です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1624602-30-7
Sample solution is provided at 25 µL, 10mM.
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VR23 is an effective proteasome inhibitor, with IC50 values of 3 μmol/L, 1 nmol/L, and 50-100 nmol/L to inhibit activities of caspase-like proteasomes, trypsin-like proteasomes, and chymotrypsin-like proteasomes, respectively [1].
As a regulator, the ubiquitin-proteasome system is important for cell growth and apoptosis [2]. The ubiquitin-proteasome pathway is critical in the regulated degradation of proteins involved in tumor growth and cell cycle control [3].
Treatment with VR23 made cancer cells undergo an abnormal centrosome amplification cycle. This cycle was caused by the accumulation of ubiquitinated cyclin E. Bortezomib is clinically approved as a chymotrypsin-like proteasome inhibitor. VR23 in combinations with bortezomib, caused a synergistic effect in killing multiple myeloma cells. This synergistic effect was also effective to myeloma cells resistant to bortezomib [1].
In vivo, VR23 was effective in controlling metastatic breast cancer cells and multiple myelomas [1]. In engrafted animals, the treatment with VR23 at 30 mg/kg twice per week for three weeks inhibited tumor growth effectively. Following 24 hours pre-treatment with paclitaxel at 20mg/kg/week, the administration of VR23 enhanced the anti-tumor activity of paclitaxel by 70%. Histological data showed that VR23 substantially decreased mitotic index, inhibited tumor infiltration into surrounding tissues and remarkably reduced tumor cell proliferation and angiogenesis [4].
References:
[1]. Pundir S, Vu HY, Solomon VR, et al. VR23: A Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E-Mediated Centrosome Amplification. Cancer research, 2015, 75(19): 4164-4175.
[2]. Almond JB, Cohen GM. The proteasome: a novel target for cancer chemotherapy. Leukemia, 2002, 16(4): 433-443.
[3]. Adams J, Palombella VJ, Sausville EA, et al. Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer research, 1999, 59(11): 2615-2622.
[4]. Vu HYT, Pundir S, Solomon RV, et al. Anticancer effects and mechanism of VR23, a novel chloroquine derivative. Cancer Research, 2014, 74(19 Supplement): 4545-4545.
| Cas No. | 1624602-30-7 | SDF | |
| Chemical Name | 7-chloro-4-(4-((2,4-dinitrophenyl)sulfonyl)piperazin-1-yl)quinoline | ||
| Canonical SMILES | ClC1=CC2=C(C(N3CCN(S(C4=C([N+]([O-])=O)C=C([N+]([O-])=O)C=C4)(=O)=O)CC3)=CC=N2)C=C1 | ||
| Formula | C19H16ClN5O6S | M.Wt | 477.88 |
| 溶解度 | ≥ 45.55mg/mL in DMSO | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0926 mL | 10.4629 mL | 20.9258 mL |
| 5 mM | 418.5 μL | 2.0926 mL | 4.1852 mL |
| 10 mM | 209.3 μL | 1.0463 mL | 2.0926 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: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)