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临床前CDMO研发化合物筛选
Sulforaphane
中文名称:萝卜硫素
CAS号:4478-93-7
分子式: C6H11NOS2 分子量: 177.29
产品形式: Free Base
研发状态: Recruiting
研发用途: Anthracycline Related Cardiotoxicity in Breast Cancer
研究机构: Texas Tech University Health Sciences Center
研发日期: June 1 2022
研发阶段: Phase 1 : Phase 2
Sulforaphane is a naturally occurring isothiocyanate derived from the consumption of cruciferous vegetables, such as broccoli, cabbage, and kale. It is an inducer of Nrf2. Sulforaphane is also an inhibitor of histone deacetylase (HDAC) and NF-κB. Sulforaphane increases heme oxygenase-1 (HO-1) and reduces the levels of reactive oxygen species (ROS). Sulforaphane induces cell cycle arrest and apoptosis.,
Azathioprine
中文名称: 硫唑嘌呤
CAS号:446-86-6
分子式: C9H7N7O2S 分子量: 277.26
产品形式: free base
研发状态: Recruiting
研发用途: Cytomegalovirus Infections; Transplant-Related Disorder
研究机构: University of Pennsylvania; Merck Sharp & Dohme LLC
研发日期: April 4 2024
研发阶段: Phase 2
Azathioprine(BW 57-322) is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.
Genistein (NPI 031L)
中文名称:染料木素
CAS号:446-72-0
分子式: C15H10O5 分子量: 270.24
产品形式: free base
研发状态: Completed
研发用途: Healthy
研究机构: Chalmers University of Technology
研发日期: September 27 2021
研发阶段: Not Applicable
Genistein (NPI 031L), a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM.
Pazopanib
中文名称: 帕唑帕尼
CAS号:444731-52-6
分子式: C21H23N7O2S 分子量: 437.52
产品形式: Free Base
研发状态: Recruiting
研发用途: Hereditary Hemorrhagic Telangiectasia; Epistaxis; Anemia; Nosebleed; HHT
研究机构: Cure HHT
研发日期: May 8 2023
研发阶段: Phase 2 : Phase 3
Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.
Vandetanib (ZD6474)
中文名称:凡德他尼
CAS号:443913-73-3
分子式: C22H24BrFN4O2 分子量: 475.35
产品形式: free base
研发状态: Completed
研发用途: Carcinoma Hepatocellular; Metastatic Colorectal Cancer
研究机构: Boston Scientific Corporation; Biocompatibles UK Ltd
研发日期: May 17 2017
研发阶段: Early Phase 1
Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).
Metronidazole
中文名称: 甲硝唑
CAS号:443-48-1
分子式: C6H9N3O3 分子量: 171.15
产品形式: free base
研发状态: Not yet recruiting
研发用途: Acute Mesenteric Ischemia
研究机构: Assistance Publique - Hôpitaux de Paris
研发日期: September 1 2024
研发阶段: Phase 3
Metronidazole, a synthetic antibacterial and antiprotozoal agent of the nitroimidazole class, is used against protozoa.
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