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临床前CDMO研发化合物筛选
Mivebresib (ABBV-075)
中文名称:米维布塞
CAS号:1445993-26-9
分子式: C22H19F2N3O4S 分子量: 459.47
产品形式: free base
研发状态: Terminated
研发用途: Myelofibrosis (MF)
研究机构: AbbVie
研发日期: March 17 2021
研发阶段: Phase 1
Mivebresib (ABBV-075) is a novel BET family bromodomain inhibitor. It binds bromodomains of BRD2/4/T with similar affinities (Ki of 1-2.2 nM) and highly selective for 18 bromodomain proteins tested (Kd > 1 μM; more than 600-fold selectivity vs. BRD4), but exhibits roughly 10-fold weaker potency towards BRD3 (Ki of 12.2 nM) and has moderate activity towards CREBBP (Kd = 87 μM; 54-fold selectivity vs. BRD4). Mivebresib(ABBV-075) efficiently triggers apoptosis in various tumor cell.
Paliperidone
中文名称: 9－羟基利培酮
CAS号:144598-75-4
分子式: C23H27FN4O3 分子量: 426.48
产品形式: free base
研发状态: Not yet recruiting
研发用途: Schizophrenia; Treatment-resistant Schizophrenia; Side Effect; Lipid Metabolism Disorders; Diabetes; NAFLD; Psychosis
研究机构: Consorcio Centro de Investigación Biomédica en Red (CIBER); Instituto de Salud Carlos III
研发日期: November 1 2023
研发阶段: Phase 4
Paliperidone, the main active metabolite of Risperidone, is a potent serotonin-2A and dopamine-2 receptor antagonist, used in the treatment of schizophrenia.
NVR 3-778
中文名称:4-氟-3-[(4-羟基-1-哌啶基)磺酰基]-N-(3,4,5-三氟苯基)苯甲酰胺
CAS号:1445790-55-5
分子式: C18H16F4N2O4S 分子量: 432.39
产品形式: Free base
研发状态: Completed
研发用途: Chronic Hepatitis B
研究机构: Novira Therapeutics Inc.
研发日期: April 30 2014
研发阶段: Phase 1
NVR 3-778, belonging to the SBA (sulfamoylbenzamide) class, is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator). NVR 3-778 exhibits anti-HBV activity.
Sodium Bicarbonate
中文名称: 碳酸氢钠
CAS号:144-55-8
分子式: CH2O3.Na 分子量: 85.01
产品形式: Free base
研发状态: Active not recruiting
研发用途: Chronic Kidney Disease Stage 5
研究机构: Osaka University
研发日期: January 1 2023
研发阶段: Not Applicable
Sodium bicarbonate(Armex Blast Media Flow Formula XL, BI-CF 40E, BI-H 40E, Bakeshure 180, Sodium Hydrogen Carbonate, Sodium hydrogen carbonate) is a biochemical reagent used as a pH buffering agent, an electrolyte replenisher, systemic alkalizer and in topical cleansing solutions.
Metarrestin (ML246)
中文名称:化合物METARRESTIN
CAS号:1443414-10-5
分子式: C31H30N4O 分子量: 474.60
产品形式: Free Base
研发状态: Recruiting
研发用途: Advanced Solid Tumors; Metastatic Pancreatic Cancer; Pediatric Solid Tumor; Advanced Breast Cancer; Malignant Peripheral Nerve Sheath Tumor; Colorectal Neoplasms
研究机构: National Cancer Institute (NCI); National Institutes of Health Clinical Center (CC)
研发日期: October 27 2020
研发阶段: Phase 1
Metarrestin (ML246) is an orally active and specific perinucleolar compartment (PNC) inhibitor that disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription. Metarrestin blocks metastatic development and extends survival in mouse cancer models.
Ripretinib (DCC-2618)
中文名称:瑞普替尼
CAS号:1442472-39-0
分子式: C24H21BrFN5O2 分子量: 510.36
产品形式: Free Base
研发状态: Withdrawn
研发用途: Gastrointestinal Stromal Tumors
研究机构: Deciphera Pharmaceuticals LLC
研发日期: Nov-21
研发阶段: Phase 1 : Phase 2
DCC-2618 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of the tumor-associated antigens (TAA) mast/stem cell factor receptor (SCFR) Kit (c-Kit) and PDGFR-alpha, with IC50 values of 4 nM, 8 nM, 18 nM, 5 nM and 14 nM for WT Kit (c-Kit), V654A Kit (c-Kit), T670I Kit (c-Kit), D816H Kit (c-Kit) and D816V Kit (c-Kit), respectively.
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