UNBS 5162 |
| رقم الكتالوجGC17538 |
UNBS 5162 هو مضاد شامل للتعبير الكيميائي CXCL ، مع نشاط مضاد للورم.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 956590-23-1
Sample solution is provided at 25 µL, 10mM.
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UNBS5162 is a pan-antagonist of CXCL chemokines. By using the MTT colorimetric assay, IC50 values of the mean antiproliferative activity against nine human cancer cell lines were 19.8 and 17.9 μ M for UNBS3157 and UNBS5162, respectively.
CXCL chemokines is composed of a CXC chemokine domain, a mucin-like stalk, a transmembrane domain and a cytoplasmic tail containing a potential tyrosine phosphorylation site that may bind SH2.
UNBS5162 display weak antiproliferative activity in vitro.
UNBS5162 increases the therapeutic benefits of taxol in the orthotopic human PC-3 prostate cancer model. The proliferation of PC-3 cell and DU-145 prostate cancer cells were prevented by 10 μM UNBS5162 in vitro after the 6-day treatment. Flow cytometry analysis revealed that treatment of PC-3 and DU-145 cells with 10 μM UNBS5162 for 72 hours markedly blocked PC-3 cells in their G2 cell cycle phase and to a lesser extent in DU-145 cells. The percentage of PC-3 cells in the G2/M phase markedly increased, and accordingly the percentage of cells in the G1 phase diminished. The Rb protein expression in PC-3 cells was completely abolished after 48 and 72 hours treatment of 10 μM UNBS5162.
The cell cycle kinetics of PC-3 or DU-145 was not significantly modified by 1 μM UNBS5162. UNBS5162 at 1 μM induced no marked modifications in Rb, pRb, and E2F1 protein expression. UNBS5162 at concentrations higher than 1 μM was toxic, as indicated by inhibited proliferation of murine and human hematopoietic stem and progenitor cells
References:
[1]. Mijatovic T, Mahieu T, Bruyère C et al. UNBS5162, a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers. Neoplasia. 2008 Jun;10(6):573-86.
Animal experiment: | Mice[1]Orthotopic xenografts are obtained by injecting 2.5 × 106 human PC-3 or DU-145 cells into the prostate of 6-week-old male nu/nu mice (n = 9 animals per treatment group). All grafts are performed under anesthesia [saline/Rompun/Imalgene; 5:1:1 by volume]. The end point in these orthotopic experiments is the survival period of the tumor-bearing mice after the administration of UNBS3157, UNBS5162, or reference anticancer agents (taxol, mitoxantrone, and amonafide). However, for ethical reasons, animals are killed when 20% of body weight have been lost compared to that determined at the time of tumor grafting. All animals are weighed three times a week. Autopsies and histologic diagnoses are performed on each mouse to confirm the presence of tumor development; 100% is achieved. In the case of UNBS5162 experiments in the PC-3 model, after the sacrifice of animals, tumors are removed from both drug-treated [10 mg/kg, intravenous (i.v.)] and vehicle-treated mice, fixed in buffered formalin, embedded in paraffin, and 5-µm-thick sections taken. These histologic slides are then stained with hematoxylin and eosin for blood vessel counts[1]. |
References: [1]. Mijatovic T, et al. UNBS5162, a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers. Neoplasia. 2008 Jun;10(6):573-86. | |
| Cas No. | 956590-23-1 | SDF | |
| Chemical Name | 1-(2-(2-(dimethylamino)ethyl)-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin-5-yl)urea | ||
| Canonical SMILES | CN(C)CCN1C(C2=C3C(C=CC=C3C1=O)=CC(NC(N)=O)=C2)=O | ||
| Formula | C17H18N4O3 | M.Wt | 326.35 |
| الذوبان | DMF: 3 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 2 mg/ml | 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. |
||
| 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 | 3.0642 mL | 15.321 mL | 30.6419 mL |
| 5 mM | 612.8 μL | 3.0642 mL | 6.1284 mL |
| 10 mM | 306.4 μL | 1.5321 mL | 3.0642 mL |
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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.
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Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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