AZ10606120 dihydrochloride

Catalog No.S3520 Batch:S352001

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Technical Data

Formula

C25H36Cl2N4O2
Molecular Weight 495.48 CAS No. 607378-18-7
Solubility (25°C)* In vitro DMSO 99 mg/mL (199.8 mM)
Water 17 mg/mL (34.31 mM)
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.)

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Biological Activity

Description AZ10606120 dihydrochloride (2HCl) is a potent and selective antagonist for P2X7 receptor (P2X7R) with IC50 of ~10 nM. AZ10606120 dihydrochloride exhibits anti-depressant effects and reduces tumour growth. This product is not soluble in PBS solution. Please do not dissolve it in PBS for administration.
Targets
P2X7R [1]
(Cell-free assay)
10 nM
In vitro

AZ10606120, a P2X7R antagonist, significantly reduces the tumour cell number in both U251 cells and human glioma samples, also more effectively inhibits tumour proliferation in U251 cells when compared with the conventional chemotherapeutic agent, temozolomide.[2]
In vivo

AZ10606120, the P2X7R allosteric inhibitor, has anti‐proliferative effects in vivo, by reducing pancreatic stellate cells (PSCs) number/activity and collagen deposition.[3]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    Glioma cells from human tumour sample , U251 human glioblastoma cell line

  • Concentrations

    5, 25 μM for U251 cells, 15 μM for human glioma samples

  • Incubation Time

    72 h

  • Method

    AZ10606120 concentrations of 5 μM and 25 μM was for U251 cells and 15 μM was for human glioma samples. For comparison of P2X7R antagonism efficacy with conventional glioma treatment, cells were also treated with the chemotherapeutic agent, temozolomide. After 72 h of treatment, cells were fixed with 1:1 acetone-methanol solution at − 20 °C for 15 min. Fixed cells were subsequently stained with 5 μM of DAPI nuclear counterstain at 25 °C for 1 h. Cells were viewed with an Olympus IX-81 fluorescence microscope, and a cell count was conducted based on the number of DAPI-positive nuclei.
Animal Study:

[3]
  • Animal Models

    Orthotopic xenograft mouse model of pancreatic ductal adenocarcinoma (PDAC)

  • Dosages

    5 mg/kg

  • Administration

    i.p.

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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.