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Technical Data
| Formula | C22H22FN3O3 |
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| 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 | |||
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* <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 | AZD2461 is a novel PARP inhibitor with low affinity for Pgp than Olaparib. Phase 1. | |
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| In vitro | AZD2461 has lower affinity for Pgp than does Olaparib. [1] | |
| In vivo | AZD2461 has an 80-fold increased Mdr1b expression on Olaparib-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] |
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Customer Product Validation
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Data from [Data independently produced by , , Cell Death Differ, 2017, 24(6):1091-1099]
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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.