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临床前CDMO研发化合物筛选
Citarinostat (ACY-241)
中文名称:2-[(2-氯苯基)苯基氨基]-N-[7-(羟基氨基)-7-氧代庚基]-5-嘧啶甲酰胺
CAS号:1316215-12-9
分子式: C24H26ClN5O3 分子量: 467.95
产品形式: free base
研发状态: Completed
研发用途: Malignant Melanoma
研究机构: Celgene; Syneos Health; ApoCell Inc.; Celerion; NYU Langone Health
研发日期: September 30 2016
研发阶段: Phase 1
Citarinostat (ACY-241, HDAC-IN-2) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.
Ricolinostat (ACY-1215)
CAS号:1316214-52-4
分子式: C24H27N5O3 分子量: 433.50
产品形式: free base
研发状态: Completed
研发用途: Metastatic Breast Cancer; Breast Carcinoma
研究机构: Columbia University; Acetylon Pharmaceuticals Incorporated; National Cancer Institute (NCI)
研发日期: March 1 2016
研发阶段: Phase 1
Ricolinostat (ACY-1215, Rocilinostat) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Ricolinostat (ACY-1215) suppresses cell proliferation and promotes apoptosis. Phase 2.
N-Acetylneuraminic acid
中文名称:N-乙酰神经氨酸
CAS号:131-48-6
分子式: C11H19NO9 分子量: 309.27
产品形式: free base
研发状态: Completed
研发用途: N-Acetylneuraminic Acid Storage Disease
研究机构: University of Lausanne; University of Modena and Reggio Emilia
研发日期: May 1 2018
研发阶段: Not Applicable
N-Acetylneuraminic acid (Neu5Ac, NeuAc, Acido aceneuramico, Acide aceneuramique, Acidium aceneuramicum, Sialic acid, NANA) is the predominant sialic acid found in mammalian cells. Sialic acids are negatively charged monosaccharides attached to the end of sugar chains, giving rise to a wide variety of glycoproteins and glycolipids in biological fluids and cell membranes.
Miransertib (ARQ 092) HCl
中文名称:ARQ092盐酸盐
CAS号:1313883-00-9
分子式: C27H25ClN6 分子量: 468.98
产品形式: hydrochloride
研发状态: Completed
研发用途: Solid Tumor; Malignant Lymphoma; Tumor
研究机构: ArQule Inc. a subsidiary of Merck Sharp & Dohme LLC a subsidiary of Merck & Co. Inc. (Rahway NJ USA)
研发日期: Nov-11
研发阶段: Phase 1
Miransertib (ARQ 092) HCl is a novel, orally bioavailable and selective AKT pathway inhibitor exhibiting a manageable safety profile among patients with advanced solid tumors.
Miransertib (ARQ-092)
中文名称:3-[3-[4-(1-氨基环丁基)苯基]-5-苯基-3H-咪唑并[4,5-b]吡啶-2-基]-2-吡啶胺
CAS号:1313881-70-7
分子式: C27H24N6 分子量: 432.52
产品形式: free base
研发状态: Completed
研发用途: Solid Tumor; Malignant Lymphoma; Tumor
研究机构: ArQule Inc. a subsidiary of Merck Sharp & Dohme LLC a subsidiary of Merck & Co. Inc. (Rahway NJ USA)
研发日期: Nov-11
研发阶段: Phase 1
Miransertib (ARQ-092) is a potent, selective and orally bioavailable allosteric inhibitor of Akt with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively.
Savolitinib (AZD6094)
中文名称:沃利替尼
CAS号:1313725-88-0
分子式: C17H15N9 分子量: 345.36
产品形式: free base
研发状态: Completed
研发用途: Healthy Male Subjects
研究机构: AstraZeneca; Parexel
研发日期: June 2 2023
研发阶段: Phase 1
Savolitinib (Volitinib, AZD6094, HMPL-504) is a novel, potent, and selective MET inhibitor currently in clinical development in various indications, including PRCC. The IC50 values of this compound for c-Met and p-Met are 5 nM and 3 nM, respectively. It shows exquisite selectivity for c-Met over 274 kinase.
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