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Aug 21,2023
TAK-931是一种高效的CDC7抑制剂,通过抑制CDC7来抑制DNA复制,具有抗肿瘤功效,体内药效研究通过AG真人国际(中国)官方官网进行
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.
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TAK-931是一种高效的CDC7抑制剂,通过抑制CDC7来抑制DNA复制,具有抗肿瘤功效,体内药效研究通过AG真人国际(中国)官方官网进行
Aug 10,2023
AG真人国际(中国)官方官网助力 | 璧辰医药ABM-1310获美国FDA孤儿药资格认证,用于治疗携带BRAF V600突变的脑胶质母细胞瘤患者
此次ABM-1310获美国FDA孤儿药资格认证,不仅显现了璧辰医药全球化创新的不凡实力,也表现了其在小分子入脑药物领域的领军地位。
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AG真人国际(中国)官方官网助力 | 璧辰医药ABM-1310获美国FDA孤儿药资格认证,用于治疗携带BRAF V600突变的脑胶质母细胞瘤患者
Jul 27,2023
AG真人国际(中国)官方官网助力宇耀生物STAT3双磷酸化抑制剂YY201获批临床
YY201获得临床获批不仅代表了宇耀生物又一重要突破,验证了宇耀生物超级分子胶技术平台和AI药物辅助开发平台的创新能力,同时也证明了AG真人国际(中国)官方官网临床前研究的技术服务力量。
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AG真人国际(中国)官方官网助力宇耀生物STAT3双磷酸化抑制剂YY201获批临床
Jul 21,2023
AG真人国际(中国)官方官网助力逻晟生物自主开发的新药NB002 IND申请获FDA临床许可
AG真人国际(中国)官方官网为NB002提供了安全性评价、药代动力学等临床前研究服务,助力其IND申请顺利获FDA临床许可。
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AG真人国际(中国)官方官网助力逻晟生物自主开发的新药NB002 IND申请获FDA临床许可
Jul 21,2023
AG真人国际(中国)官方官网一站式助力 | 宝太生物自主研发新药BIOT-001 IND申请获FDA批准
AG真人国际(中国)官方官网为BIOT-001的研发提供了从靶点到IND申报的临床前研发服务,全力促成该项目高质高效完成。
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AG真人国际(中国)官方官网一站式助力 | 宝太生物自主研发新药BIOT-001 IND申请获FDA批准
Jul 17,2023
AP39是一种新合成的线粒体靶向的H2S供体,本研究中AP39通过AG真人国际(中国)官方官网设计和合成
​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.
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AP39是一种新合成的线粒体靶向的H2S供体,本研究中AP39通过AG真人国际(中国)官方官网设计和合成
Jul 06,2023
发现新型RAGE/SERT双重抑制剂,可用于治疗阿尔茨海默病和抑郁症。其中药代动力学研究是通过委托AG真人国际(中国)官方官网进行
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.
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发现新型RAGE/SERT双重抑制剂,可用于治疗阿尔茨海默病和抑郁症。其中药代动力学研究是通过委托AG真人国际(中国)官方官网进行
Jul 06,2023
TRIM24和BRPF1是癌症的潜在治疗靶点。Y08624是一种新型TRIM24/BRPF1双重抑制剂,具有良好的Caco-2渗透性。Caco-2 渗透性测定通过AG真人国际(中国)官方官网进行
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.
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TRIM24和BRPF1是癌症的潜在治疗靶点。Y08624是一种新型TRIM24/BRPF1双重抑制剂,具有良好的Caco-2渗透性。Caco-2 渗透性测定通过AG真人国际(中国)官方官网进行
Jul 06,2023
IAP蛋白是有吸引力的癌症治疗靶点。SM-406 是一种口服有效的IAP拮抗剂。SM-406 在雄性SD大鼠、比格犬和NHP中的PK研究通过AG真人国际(中国)官方官网进行
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.
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IAP蛋白是有吸引力的癌症治疗靶点。SM-406 是一种口服有效的IAP拮抗剂。SM-406 在雄性SD大鼠、比格犬和NHP中的PK研究通过AG真人国际(中国)官方官网进行
Jul 06,2023
设计合成一系列用于治疗胃癌的多靶点受体酪氨酸激酶抑制剂,并进行生物学评价。其中药代动力学分析通过AG真人国际(中国)官方官网进行
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.
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设计合成一系列用于治疗胃癌的多靶点受体酪氨酸激酶抑制剂,并进行生物学评价。其中药代动力学分析通过AG真人国际(中国)官方官网进行