AZD2461

Catalog No.S7029 Batch:S702901

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Technical Data

Formula

C22H22FN3O3

Molecular Weight 395.43 CAS No. 1174043-16-3
Solubility (25°C)* In vitro DMSO 79 mg/mL (199.78 mM)
Ethanol 31 mg/mL (78.39 mM)
Water 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 AZD2461 is a novel PARP inhibitor with low affinity for Pgp. Phase 1.
Targets
PARP [1]
In vitro

AZD2461 has lower affinity for Pgp. [1]

In vivo

AZD2461 has an 80-fold increased Mdr1b expression on -resistant KB1P tumor T6-28, without inhibition of Pgp. AZD2461 induces loss of 53BP1 expression in mice with KB1P tumors with short-term treatment. Long-term AZD2461 treatment is well tolerated and doubled the median relapse-free survival. [1]

Protocol (from reference)

Animal Study:

[1]

  • Animal Models

    resistant tumors from KB1PM1, KB1PM3, and KB1PM4 in female mice

  • Dosages

    100 mg/kg

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , Cell Death Differ, 2017, 24(6):1091-1099]

Data from [Data independently produced by , , J Cancer Res Clin Oncol, 2019, 145(1):137-152]

Selleck's AZD2461 has been cited by 8 publications

Histone Parylation factor 1 contributes to the inhibition of PARP1 by cancer drugs [ Nat Commun, 2021, 12(1):736] PubMed: 33531508
A small-molecule inhibitor of the BRCA2-RAD51 interaction modulates RAD51 assembly and potentiates DNA damage-induced cell death [ Cell Chem Biol, 2021, S2451-9456(21)00058-1] PubMed: 33662256
Illuminating NAD+ Metabolism in Live Cells and In Vivo Using a Genetically Encoded Fluorescent Sensor [ Dev Cell, 2020, 53(2):240-252.e7] PubMed: 32197067
Illuminating NAD+ Metabolism in Live Cells and In Vivo Using a Genetically Encoded Fluorescent Sensor. [ Dev Cell, 2020, 20;53(2):240-252] PubMed: 32197067
Response of Breast Cancer Cells to PARP Inhibitors Is Independent of BRCA Status. [ J Clin Med, 2020, 30;9(4)] PubMed: 32235451
PARP inhibitors affect growth, survival and radiation susceptibility of human alveolar and embryonal rhabdomyosarcoma cell lines [Camero S, et al. J Cancer Res Clin Oncol, 2019, 145(1):137-152.] PubMed: 30357520
Neuroprotectin D1 upregulates Iduna expression and provides protection in cellular uncompensated oxidative stress and in experimental ischemic stroke. [Belayev L, et al. Cell Death Differ, 2017, 24(6):1091-1099] PubMed: 28430183
TOPBP1Dpb11 plays a conserved role in homologous recombination DNA repair through the coordinated recruitment of 53BP1Rad9. [ J Cell Biol, 2017, 216(3):623-639] PubMed: 28228534

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.