UNBS5162

Catalog No.S8869 Batch:S886901

Print

Technical Data

Formula

C17H18N4O3

Molecular Weight 326.35 CAS No. 956590-23-1
Solubility (25°C)* In vitro DMSO 17 mg/mL (52.09 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:

[1]

  • Cell lines

    PC-3 and DU- 145 cells

  • Concentrations

    10 µM

  • Incubation Time

    72 h

  • Method

    --

Animal Study:

[1]

  • Animal Models

    Female B6D2F1 mouse

  • Dosages

    20 mg/kg (iv) or 80 mg/kg (oral)

  • Administration

    i.v. bolus injection or oral administration

Selleck's UNBS5162 has been cited by 2 publications

Metformin potentiates nephrotoxicity by promoting NETosis in response to renal ferroptosis [ Cell Discov, 2023, 9(1):104] PubMed: 37848438
Metformin potentiates nephrotoxicity by promoting NETosis in response to renal ferroptosis [ Cell Discov, 2023, 9(1):104] PubMed: 37848438

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.