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Formula | C18H20N8O2 |
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Molecular Weight | 380.40 | CAS No. | 2230820-11-6 | ||||
Solubility (25°C)* | In vitro | DMSO | 9 mg/mL (23.65 mM) | ||||
Ethanol | 3 mg/mL (7.88 mM) | ||||||
Water | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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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.) |
Description | AZD7648 is a potent inhibitor of DNA-PK with an IC50 of 0.6 nM in biochemical assay and more than 100-fold selective against 396 other kinases. | ||
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Targets |
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In vitro | AZD7648 inhibits IR-induced DNA-PK S2056 auto phosphoryalation with an IC50 = 92 nM in A549 non-small cell lung cancer (NSCLC) cells. In A549 cells, AZD7648 (≥1 µM) in combination with 2Gy IR for 48 hours leads to a significant accumulation of cells arrested in the G2/M of the cell cycle, a 4-fold increase in micronuclei formation, and 3-fold induction of γH2AX, pATM S1981 and 53BP1 foci formation compared with IR alone[2]. |
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In vivo | AZD7648 is a potent and highly selective DNA-PK inhibitor, with good crystalline solubility, permeability and metabolic stability, good bioavailability and predictable pharmacokinetics in preclinical species, and potent knockdown of pRPA and regressions in murine xenograft models when combining with AZD2281 or radiation[1]. |
Cell Assay: |
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Animal Study: |
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Different Impacts of DNA-PK and mTOR Kinase Inhibitors in Combination with Ionizing Radiation on HNSCC and Normal Tissue Cells [ Cells, 2024, 13(4)304] | PubMed: 38391917 |
Negative feedback regulation of MAPK signaling is an important driver of chronic lymphocytic leukemia progression [ Cell Rep, 2023, 42(10):113017] | PubMed: 37792532 |
Phosphatases maintain low catalytic activity of SGK1: DNA damage resets the balance in favor of phosphorylation [ J Biol Chem, 2023, S0021-9258(23)01969-5] | PubMed: 37343701 |
Synergistic cytotoxicity of fludarabine, clofarabine, busulfan, vorinostat and olaparib in AML cells [ Front Oncol, 2023, 13:1287444] | PubMed: 38074694 |
Inhibition of DNA-dependent protein kinase catalytic subunit boosts rAAV transduction of polarized human airway epithelium [ Mol Ther Methods Clin Dev, 2023, 31:101115] | PubMed: 37841417 |
Disparate pathways for extrachromosomal DNA biogenesis and genomic DNA repair [ bioRxiv, 2023, 2023.10.22.563489] | PubMed: 37961138 |
MEK inhibition overcomes chemoimmunotherapy resistance by inducing CXCL10 in cancer cells [ Cancer Cell, 2022, S1535-6108(21)00662-0] | PubMed: 35051357 |
TDP1-independent pathways in the process and repair of TOP1-induced DNA damage [ Nat Commun, 2022, 13(1):4240] | PubMed: 35869071 |
DNA-PKcs promotes fork reversal and chemoresistance [ Mol Cell, 2022, 82-20:3932-3942.e6] | PubMed: 36130596 |
Effective Radiosensitization of Bladder Cancer Cells by Pharmacological Inhibition of DNA-PK and ATR [ Biomedicines, 2022, 10(6)1277] | PubMed: 35740300 |
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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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.