UNBS 5162A pan-antagonist of CXCL chemokines CAS# 956590-23-1 |
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Quality Control & MSDS
3D structure
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| Cas No. | 956590-23-1 | SDF | Download SDF |
| PubChem ID | 16048966 | Appearance | Powder |
| Formula | C17H18N4O3 | M.Wt | 326.35 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 21.5 mg/mL (65.88 mM; Need ultrasonic and warming) | ||
| Chemical Name | [2-[2-(dimethylamino)ethyl]-1,3-dioxobenzo[de]isoquinolin-5-yl]urea | ||
| SMILES | CN(C)CCN1C(=O)C2=CC=CC3=CC(=CC(=C32)C1=O)NC(=O)N | ||
| Standard InChIKey | WCKZRLOUKYFJDY-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C17H18N4O3/c1-20(2)6-7-21-15(22)12-5-3-4-10-8-11(19-17(18)24)9-13(14(10)12)16(21)23/h3-5,8-9H,6-7H2,1-2H3,(H3,18,19,24) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | UNBS5162 is a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers; the mean antiproliferative activity IC50 value is 17.9 uM for 9 cancer cell lines; hydrolysis product of UNBS3157.
IC50 value: 4.7-46.5 uMcancer cell line) [1]
Target: CXCL regulator
in vitro: The mean antiproliferative activity IC50 values determined against nine human cancer cell lines investigated (using the MTT colorimetric assay) were 19.8 and 17.9 μM for UNBS3157 and UNBS5162, respectively [1].
in vivo: In the PC-3 model, UNBS3157 displayed appreciable activity against PC-3 prostate carcinoma when administered orally at 160 mg/kg (%T/C: 151%, P = .03) but not at the lower dose of 40 mg/kg (%T/C: 100%). Repeat i.v. administration of the compound at 10 mg/kg (three times a week for 6 consecutive weeks) contributed therapeutic benefits that were similar to repeat i.v. administration (once a week for 6 consecutive weeks) of 20-mg/kg taxol in the PC-3 orthotopic model [1]. UNBS5162 was administered in a 3 + 3 dose escalation scheme by intravenous infusion over 1 h weekly for 3 weeks of a 4-week cycle. Safety, serial serum PK and tolerability were captured throughout the study. Response Evaluation Criteria in Solid Tumors was utilized every 2 cycles to assess for anti-tumor response [2]. References: | |||||
UNBS 5162 Dilution Calculator
UNBS 5162 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.0642 mL | 15.321 mL | 30.6419 mL | 61.2839 mL | 76.6049 mL |
| 5 mM | 0.6128 mL | 3.0642 mL | 6.1284 mL | 12.2568 mL | 15.321 mL |
| 10 mM | 0.3064 mL | 1.5321 mL | 3.0642 mL | 6.1284 mL | 7.6605 mL |
| 50 mM | 0.0613 mL | 0.3064 mL | 0.6128 mL | 1.2257 mL | 1.5321 mL |
| 100 mM | 0.0306 mL | 0.1532 mL | 0.3064 mL | 0.6128 mL | 0.766 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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