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临床前CDMO研发化合物筛选
Tomivosertib (eFT-508)
中文名称:6'-[(6-氨基-4-嘧啶基)氨基]-8'-甲基螺[环己烷-1,3'(2'H)-咪唑并[1,5-A]吡啶]-1',5'-二酮
CAS号:1849590-01-7
分子式: C17H20N6O2 分子量: 340.38
产品形式: free base
研发状态: Recruiting
研发用途: Acute Myeloid Leukemia
研究机构: Northwestern University; National Cancer Institute (NCI); EFFECTOR Therapeutics Inc.
研发日期: September 29 2023
研发阶段: Phase 1
Tomivosertib (eFT-508) is a potent and selective MNK1/2 inhibitor with IC50s of 2.4 nM and 1 nM, respectively. It potentially results in decreased tumor cell proliferation and tumor growth. Tomivosertib (eFT-508) inhibits eIF4E phosphorylation and dramatically downregulates PD-L1 protein abundance.
Mobocertinib (TAK788)
中文名称:莫博替尼/TAK-788
CAS号:1847461-43-1
分子式: C32H39N7O4 分子量: 585.70
产品形式: Free Base
研发状态: Withdrawn
研发用途: Non-small Cell Lung Cancer (NSCLC)
研究机构: Takeda
研发日期: March 30 2024
研发阶段: --
Mobocertinib (TAK788, AP32788), an investigational TKI, is a potent, selective preclinical inhibitor of epidermal growth factor receptor (EGFR) and HER2 mutations. Mobocertinib (TAK788) is an antineoplastic agent.
Gefitinib (ZD1839)
中文名称:吉非替尼
CAS号:184475-35-2
分子式: C22H24ClFN4O3 分子量: 446.90
产品形式: free base
研发状态: Terminated
研发用途: Non Small Cell Lung Cancer
研究机构: Daiichi Sankyo Co. Ltd.; Daiichi Sankyo
研发日期: September 21 2018
研发阶段: Phase 1
Gefitinib (ZD-1839, Iressa) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.
Erlotinib (OSI-774)
中文名称:埃罗替尼
CAS号:183321-74-6
分子式: C22H23N3O4 分子量: 393.44
产品形式: free base
研发状态: Not yet recruiting
研发用途: Cirrhosis Liver
研究机构: University of Texas Southwestern Medical Center; National Cancer Institute (NCI)
研发日期: Jul-24
研发阶段: Phase 2
Erlotinib (OSI-774, CP358774, NSC 718781, Tarceva) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.
Erlotinib (OSI-774) HCl
中文名称:盐酸埃罗替尼
CAS号:183319-69-9
分子式: C22H23N3O4.HCl 分子量: 429.90
产品形式: Hydrochloride
研发状态: Not yet recruiting
研发用途: Cirrhosis Liver
研究机构: University of Texas Southwestern Medical Center; National Cancer Institute (NCI)
研发日期: Jul-24
研发阶段: Phase 2
Erlotinib (OSI-774, CP358774, NSC 718781) HCl is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.
Clindamycin
中文名称:克林霉素
CAS号:18323-44-9
分子式: C18H33ClN2O5S 分子量: 424.98
产品形式: Free Base
研发状态: Completed
研发用途: Acne Vulgaris
研究机构: Jinnah Postgraduate Medical Centre
研发日期: August 1 2022
研发阶段: Phase 2
Clindamycin inhibits protein synthesis by acting on the 50S ribosomal, used for the treatment of bacterial infections.
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