UNBS 5162

A pan-antagonist of CXCL chemokines CAS# 956590-23-1

UNBS 5162

Catalog No. BCC4008----Order now to get a substantial discount!

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UNBS 5162: 5mg $115 In Stock
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Chemical structure

UNBS 5162

3D structure

Chemical Properties of UNBS 5162

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.
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.
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.

Biological Activity of UNBS 5162

DescriptionUNBS5162 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:
[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. [2]. Mahadevan D, et al. Phase I trial of UNBS5162, a novel naphthalimide in patients with advanced solid tumors or lymphoma. Int J Clin Oncol. 2013 Oct;18(5):934-41.

UNBS 5162 Dilution Calculator

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UNBS 5162 Molarity Calculator

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Preparing Stock Solutions of UNBS 5162

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.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

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Yale University

Worcester Polytechnic Institute

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Universidade da Beira Interior

The Institute of Cancer Research

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The University of Michigan
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Universite de Paris
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Auckland University
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The University of Tokyo
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Background on UNBS 5162

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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UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.

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