Jun 11,2025

MGST1過表達通過激活Akt/GSK-3β信號通路誘導胃癌細胞增殖，本研究中MGST1過表達等體外實驗通過尊龍凱時進行

Gastric cancer (GC) is one of the most common malignancies and is the leading global cause of death by cancer. Over recent decades, targeted therapies and immunotherapy have become significant new approaches for the treatment of GC. Ferroptosis is a newly verified form of modulated cell death that is characterized by lipid peroxidation. Further exploration of the function of ferroptosis in the progression of GC has provided novel opportunities for diagnosis and treatment. The overexpression of MGST1 induced the activation of the Akt/GSK-3β pathway. An Akt inhibitor antagonized the inhibitory effects of MGST1 on autophagy and ferroptosis. MGST1 and ATG16L1 overexpression, and MGST1 depletion assay were conducted by Medicilon.

Jun 11,2025

通過聯合治療提高免疫療法療效，本研究中臨床前體內藥效研究通過尊龍凱時進行

Cell division cycle 7 (CDC7), a serine/threonine kinase, plays important roles in the initiation of DNA replication. TAK-931, a highly specific CDC7 inhibitor, acts as a next-generation of replication stress (RS) inducer. Combination treatment with TAK-931 and immune checkpoint inhibitors (ICIs) enhances antiproliferative activities in preclinical syngeneic mouse models. The flowcytometry (FCM)-based immune profiling panel studies in J558 allograft syngeneic mouse models were performed at Medicilon. In vivo efficacy studies in J558 allograft models in combination with anti-mPD-1, anti-mPD-L1, and anti-mCTLA-4 antibodies were performed at Medicilon. Therapeutic potential of TAK-931 in antitumor efficacy and immunity, which may improve clinical benefit of the currently-used immunotherapy by combination treatment.

Jun 10,2025

一種有望治療非酒精性脂肪性肝病 (NAFLD) 的潛在藥物，本研究中臨床前急性毒性評估通過尊龍凱時進行

Chrysin is a natural flavonoid that has been reported as a potential treatment for non-alcoholic fatty liver disease (NAFLD). Researchers synthesized a novel chrysin derivative prodrug (C-1) and further investigated its potential therapeutic mechanism against NAFLD in vitro and in vivo. C-1 had a low toxicity profile. Their data demonstrated that C-1 may be a promising agent for NAFLD therapy. Evaluation experiments of the acute toxicities of C-1 were conducted by Medicilon.

Aug 21,2023

TAK-931是一種高效的CDC7抑制劑，通過抑制CDC7來抑制DNA復制，具有抗腫瘤功效，體內藥效研究通過尊龍凱時進行

Replication stress (RS) is a cancer hallmark; chemotherapeutic drugs targeting RS are widely used as treatments for various cancers. To develop next-generation RS-inducing anticancer drugs, cell division cycle 7 (CDC7) has attracted attention as a target. Researchers have developed an oral CDC7-selective inhibitor, TAK-931, as a candidate clinical anticancer drug. TAK-931 demonstrated marked, dose-dependent antitumor activity, without severe body weight loss. Antitumor efficacy studies for TAK-931 were carried out in two pancreatic PDX models, PHTX-249Pa and PHTXM-97Pa, at Medicilon.

Jul 17,2023

AP39是一種新合成的線粒體靶向的H2S供體，本研究中AP39通過尊龍凱時設計和合成

?Alzheimer's disease (AD) is the most universal age-related neurodegenerative disease. AP39 is a newly synthesized mitochondrially targeted H2S donor on mitochondrial function. AP39 increases intracellular H2S levels, mainly in mitochondrial regions. AP39 exerts dose-dependent effects on mitochondrial activity in APP/PS1 neurons. AP39, a novel mitochondria-targeted H2S donor, was designed and synthesized by Medicilon.

Jul 06,2023

發現新型RAGE/SERT雙重抑制劑，可用于治療阿爾茨海默病和抑郁癥。其中藥代動力學研究是通過委托尊龍凱時進行

Alzheimer's disease (AD) is a progressive and devastating neurodegenerative disorder, characterized by the presence of β-amyloid (Aβ) peptide plaques, neurofibrillary tangles, and neuroinflammation. Receptor for advanced glycation end products (RAGE) belongs to the immunoglobulin superfamily, which functions as a cell surface acceptor for Aβ peptide. RAGE plays an important role in the Aβ-mediated neuronal damage that closely related to the pathogenesis of AD. In this study, Compound 12 showed good dual-target bioactivities against RAGE and SERT in vitro, good liver microsomal stability, and acceptable pharmacokinetic properties. Pharmacokinetic studies were commissioned by Medicilon.

Jul 06,2023

TRIM24和BRPF1是癌癥的潛在治療靶點。Y08624是一種新型TRIM24/BRPF1雙重抑制劑，具有良好的Caco-2滲透性。Caco-2 滲透性測定通過尊龍凱時進行

TRIM24 (tripartite motif-containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are epigenetics “readers”and potential therapeutic targets for cancer and other diseases. Y08624 (Compound 20l) is a new TRIM24/BRPF1 dual inhibitor. Y08624 displays reasonable Caco-2 permeability. Caco-2 permeability assay was performed by Medicilon.

Jul 06,2023

IAP蛋白是有吸引力的癌癥治療靶點。SM-406 是一種口服有效的IAP拮抗劑。SM-406 在雄性SD大鼠、比格犬和NHP中的PK研究通過尊龍凱時進行

Apoptosis is a cellular process critical to the normal development and homeostasis of multicellular organisms. The inhibitor of apoptosis proteins (IAPs) are a class of key apoptosis regulators. IAP proteins are attractive cancer therapeutic targets. SM-406 (compound 2) is a potent and orally bioavailable antagonist of the IAPs. Pharmacokinetic (PK) studies of SM-406 (compound 2) in male Sprague Dawley rats, beagle dogs and cynomolgus monkeys (non-human primates) were performed by the Division of Pharmacokinetics and Metabolism, Medicilon. SM-406 (compound 2) has an excellent PK profile and good oral bioavailability in each of these four species.

Jul 06,2023

設計合成一系列用于治療胃癌的多靶點受體酪氨酸激酶抑制劑，并進行生物學評價。其中藥代動力學分析通過尊龍凱時進行

Gastric cancer is the second most lethal cancer across the world. Compounds 8f, inhibits FGFR1 signaling pathways as well as induces cell apoptosis, is a potential agent for the treatment of gastric cancer. The pharmacokinetical profile (PK) of 8f was tested in SD rats. Compound 8f showed an acceptable half-time of 3 h and displayed moderate maximum concentrations, which is enough to meet the concentration of the compound 8f to exert its efficacy in vivo. The pharmacokinetic analysis was performed by the testing service provided by Medicilon.

Jul 06,2023

表觀遺傳修飾，如DNA甲基化，在遺傳信息的表達中發揮著重要作用。DNA甲基轉移酶維持DNA甲基化，是腫瘤化療的一個有吸引力的靶點

Epigenetic modification, like DNA methylation, plays a major role in the expression of genetic information. The DNA methyltransferases (DNMTs), maintain DNA methylation, is an attractive target for tumor chemotherapy. WK-23 displays a good inhibitory effect on human DNMT1 with an IC50 value of 5.0?μM. The PK profile of WK-23 was obtained with quite satisfying oral bioavailability and elimination half-life. In vivo pharmacokinetic properties of WK-22, WK-23, WK-27, and DC_517 were performed by Medicilon.