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临床前CDMO研发化合物筛选
Fluvastatin (XU-62-320) Sodium
中文名称:氟伐他汀钠
CAS号:93957-55-2
分子式: C24H25FNNaO4 分子量: 433.45
产品形式: Sodium
研发状态: Completed
研发用途: Glioma
研究机构: Centre Oscar Lambret; Anticancer Fund Belgium
研发日期: Jun-14
研发阶段: Phase 1
Fluvastatin Sodium (Vastin,XU-62-320) inhibits HMG-CoA reductase activity with IC50 of 8 nM in a cell-free assay.
Pacritinib (SB1518)
中文名称:帕西替尼(SB1518)
CAS号:937272-79-2
分子式: C28H32N4O3 分子量: 472.58
产品形式: free base
研发状态: Not yet recruiting
研发用途: Myelodysplastic Syndromes
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 1 : Phase 2
Pacritinib (SB1518) is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3.
Zotiraciclib
中文名称:14-甲基-20-氧杂-5,7,14,27-四氮杂四环[19.3.1.1(2,6).1(8,12)]二十七碳-1(25),2,4,6(27),8,10,12(26),16,21,23-十烯
CAS号:937270-47-8
分子式: C23H24N4O 分子量: 372.46
产品形式: free base
研发状态: Recruiting
研发用途: Brain Tumor; Cancer
研究机构: National Cancer Institute (NCI); National Institutes of Health Clinical Center (CC)
研发日期: May 16 2023
研发阶段: Phase 1 : Phase 2
Zotiraciclib (SB1317; TG02) is a novel small molecule potent CDK/JAK2/FLT3 inhibitor, emerged with potent CDK (IC50 against CDKs 1, 2 and 9 = 9, 5 and 3 nM, respectively), FLT3 (IC50 = 19 nM) and JAK2 (IC50 = 19 nM) potency.
Tucatinib
中文名称:图卡蒂尼(伊尔比尼替尼,ONT-380)
CAS号:937263-43-9
分子式: C26H24N8O2 分子量: 480.52
产品形式: free base
研发状态: Recruiting
研发用途: Breast Cancer
研究机构: Criterium Inc.
研发日期: January 1 2024
研发阶段: Phase 2
Tucatinib (Irbinitinib, ONT-380, ARRY-380) is an oral, potent, selective, reversible and ATP-competitive small-molecule inhibitor of ErbB-2 (also called HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2, respectively in cell-based assays, showing ~500-fold selective for HER2 vs EGFR. It has potential antineoplastic activity.
GSK690693
中文名称:土大黄甙
CAS号:937174-76-0
分子式: C21H27N7O3 分子量: 425.48
产品形式: free base
研发状态: Withdrawn
研发用途: Cancer
研究机构: GlaxoSmithKline
研发日期: Apr-08
研发阶段: Phase 1
GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
OSI-027
中文名称:反式-4-[4-氨基-5-(7-甲氧基-1H-吲哚-2-基)咪唑并[5,1-f][1,2,4]三嗪-7-基]环己烷羧酸
CAS号:936890-98-1
分子式: C21H22N6O3 分子量: 406.44
产品形式: free base
研发状态: Completed
研发用途: Any Solid Tumor or Lymphoma
研究机构: Astellas Pharma Inc
研发日期: Jun-08
研发阶段: Phase 1
OSI-027 (ASP4786, CERC 006, AEVI-006) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM in cell-free assays, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. OSI-027 induces autophagy in cancer cells.
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