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临床前CDMO研发化合物筛选
Simurosertib
CAS号:1330782-76-7
分子式: C17H19N5OS 分子量: 341.43
产品形式: Free base
研发状态: Completed
研发用途: Neoplasms Advanced Solid
研究机构: Millennium Pharmaceuticals Inc.; Takeda
研发日期: March 28 2019
研发阶段: Phase 1
Simurosertib (TAK-931), an oral cell division cycle 7 (CDC7)-selective inhibitor with an IC50<0.3 nM, induces S phase delay and replication stress and causes mitotic aberrations through centrosome dysregulation and chromosome missegregation, resulting in irreversible antiproliferative effects in cancer cells.
Rifampin (NSC-113926)
中文名称:利福平
CAS号:13292-46-1
分子式: C43H58N4O12 分子量: 822.94
产品形式: free base
研发状态: Completed
研发用途: COVID-19 Pneumonia
研究机构: Zhejiang ACEA Pharmaceutical Co. Ltd.
研发日期: January 4 2023
研发阶段: Phase 1
Rifampin (NSC-113926, Rimactane, Rifampicin) is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections.
Ramosetron Hydrochloride
中文名称:盐酸雷莫司琼
CAS号:132907-72-3
分子式: C17H17N3O.HCl 分子量: 315.80
产品形式: hydrochloride
研发状态: Completed
研发用途: Diarrhea-predominant Irritable Bowel Syndrome
研究机构: Astellas Pharma Inc
研发日期: Feb-13
研发阶段: Phase 3
Ramosetron Hydrochloride (YM-060) is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity.
Olanzapine
中文名称:奥氮平
CAS号:132539-06-1
分子式: C17H20N4S 分子量: 312.44
产品形式: free base
研发状态: Not yet recruiting
研发用途: Weight Gain
研究机构: Rajavithi Hospital
研发日期: April 3 2024
研发阶段: Not Applicable
Olanzapine (LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
Benztropine mesylate
中文名称:苯扎托品
CAS号:132-17-2
分子式: C21H25NO.CH4SO3 分子量: 403.53
产品形式: Mesylate
研发状态: Terminated
研发用途: Schizophrenia; Schizoaffective Disorder; Schizophreniform Disorder; Delusional Disorder; Psychotic Disorders
研究机构: Centre for Addiction and Mental Health
研发日期: Jun-07
研发阶段: Not Applicable
Benztropine(Cogentin mesylate, Benztropine methanesulfonate) is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.
Flavopiridol (L86-8275) HCl
中文名称:夫拉平度盐酸盐
CAS号:131740-09-5
分子式: C21H20ClNO5.HCl 分子量: 438.30
产品形式: Hydrochloride
研发状态: Terminated
研发用途: Adult Lymphocyte Depletion Hodgkin Lymphoma; Adult Lymphocyte Predominant Hodgkin Lymphoma; Adult Mixed Cellularity Hodgkin Lymphoma; Adult Nodular Sclerosis Hodgkin Lymphoma; Anaplastic Large Cell Lymphoma; Angioimmunoblastic T-cell Lymphoma; Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue; Nodal Marginal Zone B-cell Lymphoma; Recurrent Adult Diffuse Large Cell Lymphoma; Recurrent Adult Diffuse Mixed Cell Lymphoma; Recurrent Adult Diffuse Small Cleaved Cell Lymphoma; Recurrent Adult Grade III Lymphomatoid Granulomatosis; Recurrent Adult Hodgkin Lymphoma; Recurrent Adult T-cell Leukemia/Lymphoma; Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma; Recurrent Grade 1 Follicular Lymphoma; Recurrent Grade 2 Follicular Lymphoma; Recurrent Grade 3 Follicular Lymphoma; Recurrent Mantle Cell Lymphoma; Recurrent Marginal Zone Lymphoma; Recurrent Mycosis Fungoides/Sezary Syndrome; Recurrent Small Lymphocytic Lymphoma; Refractory Multiple Myeloma; Splenic Marginal Zone Lymphoma; Stage I Multiple Myeloma; Stage II Multiple Myeloma; Stage III Multiple Myeloma; Waldenström Macroglobulinemia
研究机构: National Cancer Institute (NCI)
研发日期: Dec-05
研发阶段: Phase 1 : Phase 2
Flavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol HCl induces autophagy and ER stress. Flavopiridol HCl blocks HIV-1 replication. Phase 1/2.
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