AZD-7762 / AstraZeneca - LARVOL DELTA

An O-glycosylation-based prognostic signature for biochemical recurrence in prostate cancer identifies GALNTL6 as a potential promoter of malignant phenotypes. (PubMed, Transl Androl Urol) - "Drug-sensitivity analysis suggested that patients with different OGs scores may show distinct predicted responses to candidate agents, including AZD7762, a checkpoint kinase inhibitor, and tigecycline, a glycylcycline antibiotic with reported antitumor activity. This study establishes an O-glycosylation-related prognostic model for BCR risk stratification in PCa and identifies GALNTL6 as a potential promoter of malignant phenotypes. These findings suggest that GALNTL6 may be associated with AKT pathway activity and oxidative-stress-related transcriptional programs, although further mechanistic validation is required."

Journal • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Combined Inhibition of Wee1 and Checkpoint Kinases Synergistically Provokes S-Phase Progression and Mitotic Entry, and Promotes Cell Death Under Heat Stress. (PubMed, Genes Cells) - "Moreover, the combination of MK-1775 and AZD-7762 abrogated G2 arrest and enhanced HS-induced cell death in MG-63 and HSC-3 cells. These findings indicate that simultaneous inhibition of Wee1 and Chk1/2 could be a promising strategy for augmenting the therapeutic efficacy of hyperthermia."

Journal • Oncology

Repurposing AZD-7762 as a novel direct NLRP3 inhibitor for the treatment of inflammatory diseases. (PubMed, Int Immunopharmacol) - "Importantly, pharmacological administration of AZD-7762 significantly ameliorated disease severity in mouse models of NLRP3-driven diseases, including lipopolysaccharide (LPS)-induced systemic inflammation and dextran sulfate sodium (DSS)-induced colitis. Our findings reveal a novel function for AZD-7762 and suggest that it is a promising therapeutic candidate for the treatment of NLRP3-related inflammatory disorders."

Journal • Diabetes • Gastroenterology • Gastrointestinal Disorder • Immunology • Infectious Disease • Inflammation • Inflammatory Bowel Disease • Metabolic Disorders • Oncology • Septic Shock • Type 2 Diabetes Mellitus • CHEK1 • NLRP3

Rational design of active pharmaceutical ingredient-based co-assembled nanoparticles for cancer immunotherapy. (PubMed, J Control Release) - "In another case, the models launched multi-drug co-assembled nanomedicines including AZD7762 (AZD) and camptothecin (CPT) for synergistic cancer therapy. Both of the nanomedicines showed superior immune activation and antitumor efficiency than the free APIs. This study provides a ML-aided workflow to accelerate the design of co-assembled nanomedicines and offers feasible strategies to enhance the efficacy of anti-tumor therapies."

Journal • Breast Cancer • Immunology • Oncology • Solid Tumor • Triple Negative Breast Cancer

AI-driven multi-omics drug repurposing nominates AZD7762 as a multitarget inhibitor of IL22RA1 and FAM221A in esophageal squamous cell carcinoma. (PubMed, NPJ Precis Oncol) - "Single-cell RNA sequencing analysis mapped the hub genes interleukin 22 receptor subunit alpha 1 (IL22RA1) and family with sequence similarity 221 member A (FAM221A) to epithelial cell populations and associated them with proliferative and DNA repair programs, supporting their role in tumor progression, supporting their role in ESCC progression. In vitro assays confirmed that IL22RA1 and FAM221A promote ESCC cell proliferation, migration, and invasion. Taken together, this AI-driven multi-omics framework delivers a prognostic model, defines biologically distinct ESCC subgroups, and nominates AZD7762 as a rational multitarget drug repurposing candidate, providing a precision oncology strategy."

Journal • Esophageal Cancer • Esophageal Squamous Cell Carcinoma • Oncology • Squamous Cell Carcinoma • IL22

Simultaneous inhibition of DNA-PKcs and 53BP1 enables highly efficient Cas9-mediated insertion of genes up to 7 kb in primary cells (ASGCT 2026) - "We screened previously reported compounds that inhibit DNA-PKcs in NHEJ (AZD7648), polymerase theta in MMEJ (PolQi2), and other DNA repair pathway proteins including 53BP1 (HEP), ATR (VE822), and checkpoint kinases (AZD7762). Statistical significance determined using one-way ANOVA followed by Tukey's. ***p<0.001."

Genetic Disorders • CFTR • NOS3 • TP53BP1

ADGRF4 and ADGRL4 as novel prognostic biomarkers and potential therapeutic implications in stomach adenocarcinoma. (PubMed, BMC Gastroenterol) - "ADGRF4 and ADGRL4 were significantly overexpressed in STAD and independently associated with poor prognosis. Expression of these genes was correlated with changes in tumor microenvironment and immune cell infiltration, indicating their potential association in STAD progression. These findings suggest that ADGRF4 and ADGRL4 could serve as novel prognostic biomarkers with potential therapeutic significance in gastric cancer."

Biomarker • Journal • Gastric Adenocarcinoma • Gastric Cancer • Oncology • Solid Tumor • ELTD1

System biological approach identifies heterochromatin modification as an important mechanism of acquired cancer radioresistance (AACR 2025) - "Simultaneously, parallel high-throughput drug screening of our RR and WT cancer cells identified susceptibility to Panobinostat (Pano) - a pan-HDAC inhibitor in vitro and validated in vivo. Combinatorial Pano and AZD7762 - a Chk1 inhibitor exhibited stronger anti-tumor activity against the RR than WT cells (IC50: 0.45 nm [RR] vs 0.60 nm [WT])...Finally, knockdown of class I and II HDACs pointed to reversal of HDAC6 expression as the primary target of Pano. Herein, our systems approach of investigations of our RR cancer models uncovered the importance of the heterochromatin in acquired cancer radioresistance, and presented a potential new molecular vulnerability of RR cancer cells to targeting by epigenetic drugs."

Oncology • Prostate Cancer • CTSD • HDAC6 • JAK1 • RAD51 • RAD51AP1 • SMC1A

Combinatorial drug screen identifies therapeutic vulnerabilities of pancreatic cancer subtypes (ESMO-TAT 2026) - "decitabine, oxidative stress inducer elesclomol, and mitogen-activated protein kinase kinase (MEK) inh...rabusertib and AZD7762 ranked among the top combinations with AZD3965...adavosertib also sparked interest, as CHK1 and WEE1 inh... This systematic approach identifies candidate drug pairs for further preclinical testing and highlights translational starting points for developing personalized combination therapies to overcome resistance."

Colon Cancer • Colorectal Cancer • Oncology • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Solid Tumor • CHEK1 • SLC16A1

COMPOUND SCREEN IDENTIFIES AZD7762 AS A HIGHLY POTENT INHIBITOR OF MULTI-DRUG RESISTANT PDGFRA AND KIT AP/AL MUTATIONS (CTOS 2025) - No abstract available

Gastrointestinal Stromal Tumor • Oncology • PDGFRA

Differential Response to ATR/Chk1 Inhibition in Preleukemia and Transformed Leukemia in an MLL-ENL Model of Leukemogenesis Reflects Enrichment for Myc-Transcriptional Program (ASH 2024) - "We hypothesize that in preleukemia, ATR/Chk1 DNA damage response (DDR) checkpoint activation serves as part of intrinsic anti-cancer barrier, while in leukemia, ATR-dependent signaling is essential for leukemia cell proliferation and survival.We tested the consequences of ATR/Chk1 inhibition during Mll-ENL leukemogenesis, using ceralasertib (ATRi1, p.o. 25 mg/kg), elimusertib (ATRi2, p.o. 50 mg/kg) and AZD-7762 (Chk1i, i.v. 25 mg/kg), 3-5 times weekly, 1-6 months, using the preleukemic mice...In vitro, MEER cells showed high sensitivity to JAK2i ruxolitinib (RX, IC50 24 nM), higher than to the tested FLT3i...In preleukemia, attenuation of ATR/Chk1 checkpoint promotes the development of leukemia from preleukemia. Combinatory targeting of DDR components and activated oncogenic signaling to induce synthetic lethality in preleukemia stage of MLL remains to be fully elucidated."

Hematological Malignancies • Leukemia • Myelodysplastic Syndrome • Oncology • AMBRA1 • CHEK2 • FLT3

Identification of telomere maintenance related biomarkers and regulatory mechanisms in chronic obstructive pulmonary disease by machine learning algorithm. (PubMed, Sci Rep) - "Molecular docking showed that the TOP5 small drug molecules acting with CHEK1 were U-0126, KN-62, BX-912, LY-294,002 and AZD-7762. The results of real-time reverse transcriptase-polymerase chain reaction (RT-qPCR) showed that there were significant differences in the expression of SNRNP70 and RAD52 between COPD and control samples (p < 0.05)."

Biomarker • Journal • Chronic Obstructive Pulmonary Disease • Hepatology • Immunology • Metabolic Dysfunction-Associated Steatotic Liver Disease • Pulmonary Disease • Respiratory Diseases • CHEK1 • RAD51 • RAD52 • SNRNP70

WD40 Protein NLE1 as a Novel Diagnostic Biomarker Promoting Hepatocellular Carcinoma Proliferation. (PubMed, Clin Med Insights Oncol) - "Through organoid response characterization, we also found a significant correlation between NLE1 expression and sensitivity to the small molecules 17-AAG, AZD7762, and JQ1. Finally, enrichment analysis and proliferation assays confirmed that elevated NLE1 expression promotes HCC cell proliferation. NLE1 is an independent diagnostic and prognostic biomarker that promotes the proliferation of HCC."

Biomarker • Journal • Hepatocellular Cancer • Liver Cancer • Oncology • Solid Tumor

A holistic computational exploration of AZD7762 as a potent selective modulator of LXRα, LXRβ and FXR: An underexplored pathway in cancer therapeutics. (PubMed, Comput Biol Med) - "These findings position C144 (AZD7762) as a promising anticancer candidate targeting LXRα, LXRβ, and FXR pathways. Further optimization and validation through in vitro and in vivo studies are essential for advancing these findings toward clinical application."

Journal • Oncology

Integrated multi-omics analysis and machine learning refine molecular subtypes and clinical outcome for hepatocellular carcinoma. (PubMed, Hereditas) - "Encouragingly, we observed that the high-CMLBS patients may exhibit increased sensitivity to Alpelisib, AZD7762, BMS-536,924, Carmustine, and GDC0810, whereas they may demonstrate reduced sensitivity to Axitinib, AZD6482, AZD8055, Entospletinib, GSK269962A, GSK1904529A, and GSK2606414, suggesting that CMLBS may contribute to the selection of chemotherapeutic agents for HCC patients. Therefore, in-depth examination of data from multi-omics data can provide valuable insights and contribute to the refinement of the molecular classification of HCC. In addition, the CMLBS model demonstrates potential as a screening tool for identifying HCC patients who may derive benefit from immunotherapy, and it possesses practical utility in the clinical management of HCC."

Clinical data • Journal • Hepatocellular Cancer • Oncology • Solid Tumor

Combinatorial functionomics identifies HDAC6-dependent molecular vulnerability of radioresistant head and neck cancer. (PubMed, Exp Hematol Oncol) - "We have uncovered HDAC6 as a promising molecular vulnerability that should be explored to treat RR-HNC."

Journal • Head and Neck Cancer • Oncology • Solid Tumor

A novel risk model consisting of nine platelet-related gene signatures for predicting prognosis, immune features and drug sensitivity in glioma. (PubMed, Hereditas) - "Nine platelet-related prognostic genes identified as prognostic signatures for glioma were closely associated with the TME and may aid in directing the clinical treatment and prognosis of gliomas."

Biomarker • Gene Signature • Journal • Brain Cancer • CNS Tumor • Glioma • Oncology • Solid Tumor • KIF20A • SULF2 • TAGLN2

Pan-cancer analysis of oncogenic role of CEP55 and experiment validation in clear cell renal cell carcinoma. (PubMed, Sci Rep) - "We also used Gene Set Cancer Analysis (GSCA) to predict a serious of small molecule CEP55 targeted drugs, such as AZ628, SB52334, SB590885, A-770,041, AZD7762, Elesclomol, panobinostat, BRD-A94377914, and LRRK2-IN-1. Our study indicated that CEP55 overexpression in most caner types was associated with poor prognosis. Notably, CEP55 was closely relevant to immune cell infiltration and impacted the response to immunotherapy and small molecule drugs against cancers."

IO biomarker • Journal • Pan tumor • Clear Cell Renal Cell Carcinoma • Genito-urinary Cancer • Oncology • Solid Tumor • CCNA2 • CD4 • CDK1 • CEP55 • KIF11 • LRRK2 • PCNA

Evaluation of BBB permeable Wee1 and Chk1 inhibitors in combination with standard of care for the treatment of glioblastoma (EANO 2024) - "Current therapies such as temozolomide (TMZ) chemotherapy exert suboptimal efficacy, necessitating new therapies such as those targeting nuclear kinases, Wee1 and Chk1...Previous studies combining commercially available Wee1 inhibitor AZD1775 and Chk1 inhibitor AZD7762 showed synergism in melanoma cells... Our novel BBB-permeable Wee1 and Chk1 inhibitors show synergism inducing higher cell kill in patient-derived G7 GBM stem-like cells. Combinations will next be tested with radiation to deduce radiosensitisation effects. With synergism observed between novel BBB-penetrant Wee1 and Chk1 inhibitors, these drugs show potential in becoming viable new therapies for GBM treatment."

Combination therapy • Brain Cancer • CNS Tumor • Glioblastoma • Melanoma • Oncology • Solid Tumor • CDK1 • GNRP • RASGRF1

Development of a Novel CD8+ T Cell-Associated Signature for Prognostic Assessment in Hepatocellular Carcinoma. (PubMed, Cancer Control) - "The CD8+ T-cell-associated signature is expected to be a tool for optimizing individual patient decision-making and monitoring protocols, and to provide new ideas for treatment and prognostic assessment of HCC."

Biomarker • IO biomarker • Journal • Retrospective data • Gastrointestinal Cancer • Hepatocellular Cancer • Oncology • Solid Tumor • ANXA2 • CD7 • CD8 • FABP5 • GZMH • IL7R • KLRB1 • RGS2

Identification of novel neuroprotectants against vincristine-induced neurotoxicity in iPSC-derived neurons. (PubMed, Cell Mol Life Sci) - "Six compounds showed favorable pharmacological profiles - AZD7762, A-674563, Blebbistatin, Glesatinib, KW-2449, and Pelitinib, all novel neuroprotectants against vincristine toxicity to neurons. In this study, we utilized high-throughput screening of a large library of compounds in a therapeutically relevant assay. We identified several novel compounds that are efficacious in protecting different neuronal subtypes from the toxicity induced by a common chemotherapeutic agent, vincristine which could have therapeutic potential in the clinic."

Journal • Breast Cancer • CNS Disorders • Hematological Malignancies • Leukemia • Oncology • Osteosarcoma • Pain • Sarcoma • Solid Tumor

m6A- and m5C- modified lncRNAs orchestrate the prognosis in cutaneous melanoma and m6A- modified LINC00893 regulates cutaneous melanoma cell metastasis. (PubMed, Skin Res Technol) - "We made an analysis of m6A- and m5C- related lncRNAs in melanoma samples and a prediction of these lncRNAs' role in prognosis, tumor microenvironment, immune infiltration, and clinicopathological features. We also found that LINC00893, which is potentially regulated by m6A modification, could serve as a tumor-suppressor in melanoma and play an inhibitory role in melanoma metastasis."

Biomarker • Journal • Cutaneous Melanoma • Melanoma • Oncology • Solid Tumor • AGAP2-AS1 • METTL3 • MIAT • SEMA6A • YTHDF3

Identification of novel neuroprotectants against vincristine-induced neurotoxicity in iPSC-derived neurons. (PubMed, Res Sq) - "Six compounds showed favorable pharmacological profiles - AZD7762, A-674563, Blebbistatin, Glesatinib, KW-2449, and Pelitinib, all novel neuroprotectants against vincristine toxicity to neurons. In this study, we utilized high-throughput screening of a large library of compounds in a therapeutically relevant assay. We identified several novel compounds that are efficacious in protecting different neuronal subtypes from the toxicity induced by a common chemotherapeutic agent, vincristine which could have therapeutic potential in the clinic."

Journal • Breast Cancer • CNS Disorders • Hematological Malignancies • Leukemia • Oncology • Osteosarcoma • Pain • Sarcoma • Solid Tumor

Developing targeted therapies for neuroblastoma by dissecting the effects of metabolic reprogramming on tumor microenvironments and progression. (PubMed, Theranostics) - "AZD7762 and etoposide were identified as potent therapeutics against MPS-I and II NB, respectively. This study provides deep insights into the molecular mechanisms underlying metabolic reprogramming-mediated malignant progression of NB. It also sheds light on developing targeted medications guided by the novel precise risk prognostication approaches, which could contribute to a significantly improved therapeutic strategy for NB."

Biomarker • Journal • Tumor microenvironment • CNS Disorders • CNS Tumor • Neuroblastoma • Oncology • Psychiatry • Solid Tumor • MYCN

DIFFERENTIAL RESPONSE TO ATR/CHK1 INHIBITION IN PRELEUKEMIA AND TRANSFORMED LEUKEMIA IN AN MLL-ENL MODEL OF LEUKEMOGENESIS (EHA 2024) - " We tested the in vivo effects of the pharmacologically characterized ATR inhibitors (ATRi) AZD-6738(ceralasertib), BAY-1895344 (elimusertib) and Chk1i AZD-7762 using previously described MLL​ENL mice. First, we analyzed the in vivo consequences of ATR inhibition during preleukemia progressing to leukemia, i. e. ,early in leukemogenesis. Preleukemia cells with active MLL-ENL revealed enrichment of gene sets related toE2F targets, cell cycle checkpoints, and DNA repair. Provision of the milder ATRi ceralasertib resulted in anincrease of immature c-kit+/Mac-1+ cells in BM and spleen."

Hematological Disorders • Hematological Malignancies • Leukemia • Myelodysplastic Syndrome • Oncology • CHEK1 • CHEK2 • FLT3