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Formula | C26H31N5O3 |
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Molecular Weight | 461.56 | CAS No. | 1821428-35-6 | |
Solubility (25°C)* | In vitro | Ethanol | 2 mg/mL (4.33 mM) | |
DMSO | Insoluble | |||
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.) |
Description | AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells. | |
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In vitro | AZD0156 shows sub-nanomolar potency in cell based assays of ATM inhibition with selectivities of greater than 1000 fold over other members of the PIKK family of enzymes[1]. | |
In vivo | AZD0156 is a permeable, highly soluble compound with excellent preclinical pharmacokinetic properties including oral bioavailability. AZD0156 shows robust efficacy in mouse xenograft models after oral administration when combined with DSB inducing agents. AZD0156 is currently undergoing early clinical assessment[1]. |
In vivo DNA replication dynamics unveil aging-dependent replication stress [ Cell, 2024, S0092-8674(24)00963-2] | PubMed: 39293447 |
Tumour-intrinsic PDL1 signals regulate the Chk2 DNA damage response in cancer cells and mediate resistance to Chk1 inhibitors [ Mol Cancer, 2024, 23(1):242] | PubMed: 39478560 |
Developmental signals control chromosome segregation fidelity during pluripotency and neurogenesis by modulating replicative stress [ Nat Commun, 2024, 15(1):7404] | PubMed: 39191776 |
Synergistic Activity of DNA Damage Response Inhibitors in Combination with Radium-223 in Prostate Cancer [ Cancers (Basel), 2024, 16(8)1510] | PubMed: 38672592 |
Inhibition of ATM or ATR in combination with hypo-fractionated radiotherapy leads to a different immunophenotype on transcript and protein level in HNSCC [ Front Oncol, 2024, 14:1460150] | PubMed: 39411143 |
Afatinib or Bevacizumab in combination with Osimertinib efficiently control tumor development in orthotopic murine models of non-small lung cancer [ PLoS One, 2024, 19(6):e0304914] | PubMed: 38935790 |
Methylation of NRIP3 Is a Synthetic Lethal Marker for Combined PI3K and ATR/ATM Inhibitors in Colorectal Cancer [ Clin Transl Gastroen, 2024, 15(3):e00682] | PubMed: 38235705 |
Homology-independent targeted insertion (HITI) enables guided CAR knock-in and efficient clinical scale CAR-T cell manufacturing [ Mol Cancer, 2023, 22(1):100] | PubMed: 37365642 |
C16orf72/HAPSTR1/TAPR1 functions with BRCA1/Senataxin to modulate replication-associated R-loops and confer resistance to PARP disruption [ Nat Commun, 2023, 14(1):5003] | PubMed: 37591890 |
Galectin-9 blockade synergizes with ATM inhibition to induce potent anti-tumor immunity [ Int J Biol Sci, 2023, 19(3):981-993] | PubMed: 36778120 |
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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.
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