ceralasertib

01/01/2022 - "In summary, in this study, we show that ceralasertib and PBD SG-3199 treatment not only intrinsically target tumor cells but also extrinsically increase tumor cell immunogenicity by inducing DC activation, which is enhanced in ATM-deficient cells."
11/07/2023 - "Ceralasertib monotherapy was tolerated at 160 mg BD intermittent and associated with anti-tumor activity. "
03/01/2023 - "TAS‑102 alone exerted minimal tumor suppressive effects; however, when used in combination with AZD6738, tumor suppression was observed, suggesting that AZD6738 may increase the effectiveness of a weakly effective drug. "
01/01/2022 - "The combination of CBX-12 with ceralasertib significantly suppressed tumor growth in mouse xenografts. "
01/01/2022 - "Using mouse models and a highly sensitive LC-MS/MS assay, the pharmacokinetics of AZD6738 were studied, including dose linearity, bioavailability, metabolism, and tissue distribution in tumor-bearing mice. "

10/01/2023 - "To explore mechanisms of acquired resistance to ATRi in ovarian cancer, we characterized ATRi-resistant ovarian cancer cells generated by metronomic dosing with the clinical ATR inhibitor AZD6738. "
10/01/2023 - "Metronomic dosing of ovarian cancer cells with the ATR inhibitor AZD6738 leads to loss of CDC25A expression and resistance to ATRi treatment."
10/01/2023 - "We show that metronomic dosing of ovarian cancer cells with AZD6738 results in resistance to ATR/ Chk1 inhibitors, that loss of CDC25A expression represents a mechanism of resistance to ATRi treatment in ovarian cancer cells and identify several circulating biomarker candidates of CDC25A low, AZD6738-resistant ovarian cancer cells."
01/27/2021 - "In vitro, both chemotherapy-resistant and chemotherapy-sensitive ovarian cancer cell lines showed synergistic anti-proliferative activity with a combination treatment of belotecan and AZD6738. "
01/01/2023 - "Combination ATR (ceralasertib) and PARP (olaparib) Inhibitor (CAPRI) Trial in Acquired PARP Inhibitor-Resistant Homologous Recombination-Deficient Ovarian Cancer."

04/01/2022 - "In vivo, xenografted colorectal cancer cells treated with the AZD6738/5‑FU combination exhibited a marked decrease in proliferation compared with the 5‑FU alone group. "
04/01/2022 - "The present results suggested that AZD6738 enhanced the effect of 5‑FU in p53‑mutated colorectal cancer."
04/01/2022 - "The effects of the AZD6738/5‑FU combination were evaluated in various colorectal cancer cells (HT29, SW480, HCT116 and DLD‑1 cells) by flow cytometry (HT29 cells), western blotting (HT29 cells) and water‑soluble tetrazolium 1 assays (HT29, SW480, HCT116 and DLD‑1 cells), as well as in an experimental animal model (HT29 cells). "
04/01/2022 - "ATR inhibitor AZD6738 increases the sensitivity of colorectal cancer cells to 5‑fluorouracil by inhibiting repair of DNA damage."
04/01/2022 - "The present study examined the effect of AZD6738, a specific inhibitor of ataxia telangiectasia mutated and rad3‑related (ATR) involved in the G2 checkpoint, combined with 5‑fluorouracil (5‑FU), a central chemotherapeutic agent, on colorectal cancer cells. "

01/01/2022 - "Here, the efficacy of combining gemcitabine with the novel ATR inhibitor AZD6738 was investigated in vitro in three bladder cancer cell lines (J82, T24, and UM-UC-3 cells). "
01/01/2022 - "The combined use of gemcitabine and AZD6738 inhibited the viability and colony formation of bladder cancer cells compared to either treatment alone. "
01/01/2022 - "Combining AZD6738 with gemcitabine could therefore be useful for bladder cancer therapy."
01/01/2022 - "Ataxia telangiectasia and Rad3-related inhibition by AZD6738 enhances gemcitabine-induced cytotoxic effects in bladder cancer cells."
05/30/2022 - "Applying DNA-PK (AZD7648) and ATR (Ceralasertib) inhibitors on SCaBER, J82 and VMCUB-1 bladder cancer cell lines, we revealed sensitization upon ionizing radiation (IR), i.e., the IC50 for each drug shifted to a lower drug concentration with increased IR doses. "

11/16/2022 - "Finally, we screened AZD6738, an ataxia telangiectasia mutated and rad3-related (ATR) inhibitor, based on the expression of ARPC1B. "
07/01/2019 - "Among nine human BTC cell lines, SNU478 and SNU869 were the most sensitive to AZD6738, and showed low expression of both ataxia-telangiectasia mutated (ATM) and p53. "
08/01/2018 - "PATRIOT: A phase I study to assess the tolerability, safety and biological effects of a specific ataxia telangiectasia and Rad3-related (ATR) inhibitor (AZD6738) as a single agent and in combination with palliative radiation therapy in patients with solid tumours."
04/01/2022 - "The present study examined the effect of AZD6738, a specific inhibitor of ataxia telangiectasia mutated and rad3‑related (ATR) involved in the G2 checkpoint, combined with 5‑fluorouracil (5‑FU), a central chemotherapeutic agent, on colorectal cancer cells. "
10/01/2021 - "Upregulation of pRAD50, indicative of ataxia telangiectasia mutated (ATM) activation, was observed in tumor biopsies during ceralasertib treatment. "