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临床前CDMO研发化合物筛选
Dapagliflozin (BMS-512148)
中文名称: 达格列净
CAS号:461432-26-8
分子式: C21H25ClO6 分子量: 408.87
产品形式: free base
研发状态: Not yet recruiting
研发用途: Heart Failure
研究机构: Centre Hospitalier Universitaire Vaudois; Great Ormond Street Hospital for Children NHS Foundation Trust; University College London
研发日期: Aug-24
研发阶段: Phase 2
Dapagliflozin (BMS-512148) is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.
Rucaparib (AG-014699) phosphate
中文名称:瑞卡帕布磷酸盐
CAS号:459868-92-9
分子式: C19H18FN3O.H3PO4 分子量: 421.36
产品形式: Phosphate
研发状态: Completed
研发用途: Epithelial Ovarian Cancer; Fallopian Tube Cancer; Primary Peritoneal Cancer
研究机构: Grupo Español de Investigación en Cáncer de Ovario; Clovis Oncology Inc.
研发日期: July 29 2020
研发阶段: --
Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.
Obeticholic Acid
中文名称:奥贝胆酸
CAS号:459789-99-2
分子式: C26H44O4 分子量: 420.63
产品形式: free base
研发状态: Recruiting
研发用途: Healthy
研究机构: Universitaire Ziekenhuizen KU Leuven; Intercept Pharmaceuticals
研发日期: August 22 2022
研发阶段: Not Applicable
Obeticholic Acid (INT-747, 6-ECDCA, 6-Ethylchenodeoxycholic acid) is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Obeticholic Acid inhibits autophagy. Phase 3.
Curcumin
中文名称:姜黄素
CAS号:458-37-7
分子式: C21H20O6 分子量: 368.38
产品形式: free base
研发状态: Not yet recruiting
研发用途: Interaction
研究机构: Washington State University
研发日期: January 1 2024
研发阶段: Early Phase 1
Curcumin (Diferuloylmethane, Natural Yellow 3, Turmeric yellow) is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase（IC50~25 μM）and Histone deacetylase (HDAC); activates Nrf2 pathway and supresses the activation of NF-κB. Curcumin induces mitophagy, autophagy, apoptosis, and cell cycle arrest with antitumor activity. Curcumin reduces renal damage associated with rhabdomyolysis by decreasing ferroptosis-mediated cell death. Curcumin exhibits anti-infective properties against various human pathogens like the influenza virus, hepatitis C virus, HIV and so on.
Motesanib (AMG-706)
中文名称:莫特塞尼
CAS号:453562-69-1
分子式: C22H23N5O 分子量: 373.45
产品形式: Free Base
研发状态: Withdrawn
研发用途: Breast Cancer; Metastatic Breast Cancer; Stage IV Breast Cancer
研究机构: Sidney Kimmel Cancer Center at Thomas Jefferson University; Susan G. Komen Breast Cancer Foundation; Amgen; Thomas Jefferson University
研发日期: Dec-13
研发阶段: Phase 1 : Phase 2
Motesanib (AMG-706) is an orally bioavailable receptor tyrosine kinase inhibitor with IC50 values of 2 nM, 3 nM, 6 nM, 8 nM, 84 nM, 59 nM for VEGFR1, VEGFR2, VEGFR3, Kit, PDGFR and Ret, respectively.
CTB
CAS号:451491-47-7
分子式: C16H13ClF3NO2 分子量: 343.73
产品形式: free base
研发状态: Not yet recruiting
研发用途: SARS-CoV-2
研究机构: University of Pennsylvania
研发日期: Feb-25
研发阶段: Phase 1 : Phase 2
CTB is a p300 activator and the lowest docked energy for CTB and p300 is 7.72 kcal/mol.
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