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Formula | C20H24N6O2S |
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Molecular Weight | 412.51 | CAS No. | 1352226-88-0 | ||||
Solubility (25°C)* | In vitro | DMSO | 82 mg/mL (198.78 mM) | ||||
Ethanol | 5 mg/mL (12.12 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 | Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2. | ||
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Targets |
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In vitro | In four Kras mutant cell lines: H23, H460, A549, and H358, AZD6738 inhibits ATR kinase activity and impairs cell viability. In ATM-deficient H23 cells, AZD6738 strongly synergizes with NSC 119875 to induce rapid cell death. [1] In p53 or ATM defective cells, AZD6738 treatment results in replication fork stalls and accumulation of unrepaired DNA damage, resulting in cell death by mitotic catastrophe. [2] |
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In vivo | In nude mice bearing H460 and H23 tumors, AZD6738 (50 mg/kg, p.o.) results in tumor growth inhibition (TGI), and the the combination with NSC 119875 causes rapid regression of ATM-deficient H23 tumors. [1] In nude mice bearing LoVo xenografts, a combination of AZD6738 (50 mg/kg) + IR (2 Gy) avoids toxicity while still maintaining efficacy. [3] |
Cell Assay: |
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Animal Study: |
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Data from [Data independently produced by , , Clin Cancer Res, 2018, doi:10.1158/1078-0432.CCR-18-1346]
Data from [Data independently produced by , , J Exp Clin Cancer Res, 2018, 37(1):205]
Data from [Data independently produced by , , Sci Rep, 2017, 7:41950]
Data from [Data independently produced by , , J Dermatol Sci, 2016, 84(3):239-247]
Deregulated DNA ADP-ribosylation impairs telomere replication [ Nat Struct Mol Biol, 2024, 10.1038/s41594-024-01279-6] | PubMed: 38714889 |
H2AX promotes replication fork degradation and chemosensitivity in BRCA-deficient tumours [ Nat Commun, 2024, 15(1):4430] | PubMed: 38789420 |
Functionally-instructed modifiers of response to ATR inhibition in experimental glioma [ J Exp Clin Cancer Res, 2024, 43(1):77] | PubMed: 38475864 |
Loss of POLE3-POLE4 unleashes replicative gap accumulation upon treatment with PARP inhibitors [ Cell Rep, 2024, 43(5):114205] | PubMed: 38753485 |
ATR inhibition radiosensitizes cells through augmented DNA Damage and G2 cell cycle arrest abrogation [ JCI Insight, 2024, e179599] | PubMed: 39235982 |
KRASG 12C-inhibitor-based combination therapies for pancreatic cancer: insights from drug screening [ Mol Oncol, 2024, 10.1002/1878-0261.13725] | PubMed: 39253995 |
Diffusion of activated ATM explains γH2AX and MDC1 spread beyond the DNA damage site [ iScience, 2024, 27(9):110826] | PubMed: 39310780 |
Ruthenium drug BOLD-100 regulates BRAFMT colorectal cancer cell apoptosis through AhR/ROS/ATR signaling axis modulation [ Mol Cancer Res, 2024, 10.1158/1541-7786.MCR-24-0151] | PubMed: 39083088 |
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 |
ATR inhibition activates cancer cell cGAS/STING-interferon signaling and promotes antitumor immunity in small-cell lung cancer [ Sci Adv, 2024, 10(39):eado4618] | PubMed: 39331709 |
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