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临床前CDMO研发化合物筛选
Varenicline (CP 526555) dihydrochloride
中文名称:二盐酸伐尼克林-Chantix
CAS号:866823-63-4
分子式: C13H15Cl2N3 分子量: 284.18
产品形式: Dihydrochloride
研发状态: Withdrawn
研发用途: Vaping
研究机构: Mayo Clinic
研发日期: February 1 2023
研发阶段: Early Phase 1
Varenicline (CP 526555, Chantix, Champix,CP 526555 dihydrochloride) dihydrochloride is a potent, partial agonist of α4β2 nicotinic acetylcholine receptor (nAChR) and α3β4 nAChR with EC50 of 2.3 μM and 55 μM, respectively. Varenicline dihydrochloride is a potent, full agonist of α7 nAChRs with EC50 of 18 μM. Varenicline is a prescription medication used for smoking cessation.
(R)-(-)-Gossypol acetic acid
CAS号:866541-93-7
分子式: C30H30O8.C2H4O2 分子量: 578.61
产品形式: free base
研发状态: Recruiting
研发用途: B-cell Non Hodgkin Lymphoma
研究机构: AbClon
研发日期: March 15 2022
研发阶段: Phase 1 : Phase 2
(R)-(-)-Gossypol (AT-101) acetic acid, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM in cell-free assays; does not inhibit BIR3 domain and BID. AT-101 simultaneously triggers apoptosis and a cytoprotective type of autophagy. Phase 2.
Setipiprant (ACT-129968)
中文名称:2-(2-(1-萘甲酰基)-8-氟-1.2.3.4-四氢吡啶并[4,3-B]吲哚-5基)乙酸
CAS号:866460-33-5
分子式: C24H19FN2O3 分子量: 402.42
产品形式: Free Base
研发状态: Completed
研发用途: Seasonal Allergic Rhinitis
研究机构: Idorsia Pharmaceuticals Ltd.
研发日期: Nov-10
研发阶段: Phase 2
Setipiprant (ACT-129968, KYTH-105) is a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2) that that has been shown to have greater specificity for DP2 (CRTH2) than for DP1.
SN-38
中文名称:7-乙基-10羟基喜树碱
CAS号:86639-52-3
分子式: C22H20N2O5 分子量: 392.40
产品形式: free base
研发状态: Recruiting
研发用途: Advanced Solid Tumor
研究机构: TaiRx Inc.
研发日期: October 31 2023
研发阶段: Phase 1
SN-38 (NK012) is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy.
Belinostat (PXD101)
中文名称:贝利司他
CAS号:866323-14-0
分子式: C15H14N2O4S 分子量: 318.35
产品形式: free base
研发状态: Not yet recruiting
研发用途: Carcinoma Neuroendocrine; Tumor Neuroendocrine; Tumors Neuroendocrine; Neuroendocrine; Carcinoma; Small Cell; Receptors
研究机构: National Cancer Institute (NCI); National Institutes of Health Clinical Center (CC)
研发日期: May 15 2024
研发阶段: Phase 2
Belinostat (PXD101, NSC726630, PX-105684) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors. Belinostat (PXD101) induces autophagy.
Tideglusib (NP031112)
中文名称: 4-苄基-2-(萘-1-基)-[1,2,4]噻二唑烷-3,5-二酮
CAS号:865854-05-3
分子式: C19H14N2O2S 分子量: 334.39
产品形式: free base
研发状态: Completed
研发用途: Autism Spectrum Disorders
研究机构: Evdokia Anagnostou; Holland Bloorview Kids Rehabilitation Hospital; McMaster University; University of Western Ontario Canada; Unity Health Toronto; University of Toronto; Anagnostou Evdokia M.D.
研发日期: February 10 2016
研发阶段: Phase 2
Tideglusib (NP031112, NP-12) is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2.
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