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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.

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?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.

Alzheimer's disease (AD) is a progressive and devastating neurodegenerative disorder, characterized by the presence of ¦Â-amyloid (A¦Â) 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 A¦Â peptide. RAGE plays an important role in the A¦Â-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.

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.

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.