UNBS5162

Catalog No.S8869

UNBS5162 Chemical Structure

Molecular Weight(MW): 326.35

UNBS5162 is a pan-antagonist of CXCL chemokine expression with in vitro cytotoxic activity (IC50 range of 0.5-5 µM) against a range of human cancer cell lines including glioblastoma (Hs683 and U373MG), colorectal (HCT-15 and LoVo), non-small-cell lung (A549) and breast (MCF-7).

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Biological Activity

Description UNBS5162 is a pan-antagonist of CXCL chemokine expression with in vitro cytotoxic activity (IC50 range of 0.5-5 µM) against a range of human cancer cell lines including glioblastoma (Hs683 and U373MG), colorectal (HCT-15 and LoVo), non-small-cell lung (A549) and breast (MCF-7).
Targets
CXCL [1]
()
In vitro

Exposure of PC-3 cells to UNBS5162 (1 µM for 5 successive days) dramatically decreases the expression of the proangiogenic CXCL chemokines. UNBS5162 displays weak in vitro antiproliferative activity with IC50 values of 17.3 μM, 16 μM, 4.7 μM, 8.5 μM, 28.8 μM, 8.9 μM, 46.5 μM, 21.2 μM, 9.1 μM in PC-3, DU-145, U373-MG, Hs683, HCT-15, LoVo, MCF-7, A549 and Bx-PC-3 cells. At 10 µM UNBS5162 markedly impairs PC-3 tumor cell growth kinetics, without inducing senescence, whereas the reverse feature is observed with respect to DU-145 cells. This difference might result from their respective p53 status and/or the extent of p16 expression. At 1 µM, UNBS5162 induces no such antitumor effects. UNBS5162 at 10 µM markedly increased the levels of heterochromatin in PC-3 cells through an increase in number of histones, at least at the mRNA levels[1]. UNBS5162 has been identified to decrease levels of CXC chemokine ligand (CXCL) chemokines, including CXCL1, CXCL5 and CXCL8, in experimental prostate cancer and has a good inhibitory effect on the proliferation of tumour cells in vitro and in vivo. It inhibits cell proliferation, invasion and migration, and promote cell apoptosis, potentially through the PI3K/AKT signalling pathway in SKOV3 ovarian cancer cells[2].

In vivo

In vivo UNBS5162 after repeat administration significantly increases survival in orthotopic human prostate cancer models. In female mice for testing the pharmacokinetic profiles of UNBS5162, Systemic exposure after oral administration of 80 mg/kg is relatively low (Cmax = 510 ng/ml and AUC0-∞ = 886 ng·h/ml) reflected in an absolute bioavailability calculated to be only 3.84%. The volume of distribution (Vd) and the total clearance are estimated to be 18.9 L/kg and 3.47 L/h per kilogram, respectively. The half-life after i.v. administration of 20-mg/kg UNBS5162 is estimated to be 3.8 hours. Post-i.v. UNBS5162 plasma levels of 10 µM are only maintained for approximately 30 minutes, whereas 1-µM levels are sustained for maximally 2 hours[1].

Protocol

Cell Research:

[1]

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  • Cell lines: PC-3 and DU- 145 cells
  • Concentrations: 10 µM
  • Incubation Time: 72 h
  • Method:

    --


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Female B6D2F1 mouse
  • Formulation: 0.5% lactic acid
  • Dosages: 20 mg/kg (iv) or 80 mg/kg (oral)
  • Administration: i.v. bolus injection or oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 17 mg/mL (52.09 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 326.35
Formula

C17H18N4O3

CAS No. 956590-23-1
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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CXCR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID