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临床前CDMO研发化合物筛选
Dabigatran etexilate mesylate
中文名称:甲磺酸达比加群酯
CAS号:872728-81-9
分子式: C35H45N7O8S 分子量: 723.84
产品形式: Mesylate
研发状态: Completed
研发用途: Atrial Fibrillation
研究机构: Boehringer Ingelheim
研发日期: June 13 2016
研发阶段: --
Dabigatran etexilate mesylate (Pradaxa, BIBR 1048MS, Dabigatran etexilate methanesulfonate) is an orally active prodrug of Dabigatran which is a reversible and selective, direct thrombin inhibitor (DTI). Dabigatran selectively and reversibly inhibits human thrombin with Ki of 4.5 nM and thrombin-induced platelet aggregation with IC50 of 10 nM.
Trametinib (GSK1120212)
中文名称:曲美替尼
CAS号:871700-17-3
分子式: C26H23FIN5O4 分子量: 615.39
产品形式: free base
研发状态: Not yet recruiting
研发用途: Cancer; BRAF V600 Mutation; Melanoma; Colorectal Cancer; Thyroid Cancer; Nonsmall Cell Lung Cancer
研究机构: Xynomic Pharmaceuticals Inc.
研发日期: Dec-24
研发阶段: Phase 1 : Phase 2
Trametinib (GSK1120212, JTP-74057, Mekinist) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. Trametinib activates autophagy and induces apoptosis.
Idelalisib
中文名称:艾代拉里斯
CAS号:870281-82-6
分子式: C22H18FN7O 分子量: 415.42
产品形式: free base
研发状态: Completed
研发用途: Chronic Lymphocytic Leukaemia
研究机构: Gilead Sciences
研发日期: September 12 2018
研发阶段: --
Idelalisib (CAL-101, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy.
acalisib (GS-9820)
中文名称:PI3K抑制剂(ACALISIB)
CAS号:870281-34-8
分子式: C21H16FN7O 分子量: 401.40
产品形式: Free Base
研发状态: Completed
研发用途: Lymphoid Malignancies
研究机构: Gilead Sciences
研发日期: Nov-12
研发阶段: Phase 1
Acalisib (GS-9820, CAL-120) is a highly selective and potent p110δ inhibitor (IC50 = 14 nM) with 114- to 400-fold selectivity over the other class I PI3K enzymes and no activity against Class II and III PI3K family members or other PI3K-related proteins including mTOR and DNA-PK.
PF-00835231
CAS号:870153-29-0
分子式: C24H32N4O6 分子量: 472.53
产品形式: Free Base
研发状态: Completed
研发用途: Healthy
研究机构: Pfizer
研发日期: October 7 2021
研发阶段: Phase 1
PF-00835231 is a 3CLpro (Mpro) inhibitor that may targets SARS-CoV-2 protease 3CLpro as a potential new treatment for COVID-19.
Apilimod (STA-5326) mesylate
中文名称:阿吡莫德甲磺酸盐
CAS号:870087-36-8
分子式: C25H34N6O8S2 分子量: 610.70
产品形式: mesylate
研发状态: Completed
研发用途: Crohn''s Disease
研究机构: Synta Pharmaceuticals Corp.; National Institute of Allergy and Infectious Diseases (NIAID); National Institutes of Health (NIH)
研发日期: Nov-05
研发阶段: Phase 2
Apilimod (STA-5326) mesylate is a potent and orally-available inhibitor of the cytokines interleukin-12 (IL-12) and interleukin-23 (IL-23) with the potential to treat certain autoimmune and inflammatory diseases. Apilimod mesylate (STA-5326 mesylate) inhibits IL-12 with IC50 of 1 nM, 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs, human monocytes and mouse PBMCs, respectively. Apilimod mesylate (STA-5326 mesylate) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.
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