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临床前CDMO研发化合物筛选
DDD107498
CAS号:1469439-69-7
分子式: C27H31FN4O2 分子量: 462.56
产品形式: Free Base
研发状态: Completed
研发用途: Healthy
研究机构: Merck KGaA Darmstadt Germany
研发日期: September 15 2017
研发阶段: Phase 1
DDD107498 (M-5717, DDD-498) is a P. falciparum translation elongation factor 2 inhibitor. DDD107498 exhibits a potent and novel spectrum of antimalarial activity against multiple life-cycle stages of the Plasmodium parasite.
Adavivint (SM04690)
CAS号:1467093-03-3
分子式: C29H24FN7O 分子量: 505.55
产品形式: Free Base
研发状态: Completed
研发用途: Knee Osteoarthritis
研究机构: Biosplice Therapeutics Inc.
研发日期: November 28 2018
研发阶段: Phase 2
Adavivint (SM04690,Lorecivivint) is a potent and specific inhibitor of canonical Wnt signaling with an EC50 of 19.5 nM for inhibiting the TCF/LEF reporter. It is ∼150- to 500-fold more potent than the other known Wnt inhibitors across multiple cellular assays.
PF-06409577
中文名称:6-氯-5-[4-(1-(羟基环丁基)苯基]-1H-吲哚-3-羧酸
CAS号:1467057-23-3
分子式: C19H16ClNO3 分子量: 341.79
产品形式: free base
研发状态: Terminated
研发用途: Healthy
研究机构: Pfizer
研发日期: Nov-14
研发阶段: Phase 1
PF-06409577 is an orally bioavailable AMPK activator with EC50 of 7 nM for α1β1γ1 in the TR-FRET assay and it shows no detectable inhibition of hERG in a patch-clamp assay (100 μM) and was not an inhibitor (IC50 > 100 μM) of the microsomal activities of major human cytochrome P450 isoforms.
Pralatrexate (NSC 754230)
中文名称: 普拉曲沙
CAS号:146464-95-1
分子式: C23H23N7O5 分子量: 477.47
产品形式: free base
研发状态: Completed
研发用途: Peripheral T-Cell Lymphoma (PTCL)
研究机构: Acrotech Biopharma Inc.; Axis Clinicals Limited
研发日期: November 10 2015
研发阶段: Phase 1
Pralatrexate (NSC 754230) is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. Pralatrexate induces tumor cell apoptosis.
Flavopiridol (L86-8275)
中文名称:夫拉平度
CAS号:146426-40-6
分子式: C21H20ClNO5 分子量: 401.84
产品形式: Free Base
研发状态: Completed
研发用途: Acute Myeloid Leukemia (AML)
研究机构: AbbVie; Sumitomo Pharma America Inc.
研发日期: May 30 2018
研发阶段: Phase 1
Flavopiridol (L86-8275, Alvocidib, NSC 649890, HMR-1275) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4, CDK6, and CDK9 with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Flavopiridol induces autophagy and ER stress. Flavopiridol blocks HIV-1 replication. Phase 1/2.
Tauroursodeoxycholic Acid (TUDCA)
中文名称:牛磺熊去氧胆酸
CAS号:14605-22-2
分子式: C26H45NO6S 分子量: 499.70
产品形式: free base
研发状态: Recruiting
研发用途: Amyotrophic Lateral Sclerosis
研究机构: Humanitas Mirasole SpA; University of Ulm; University of Sheffield; University Hospital Tours; KU Leuven; UMC Utrecht; University of Dublin Trinity College; Bruschettini S.r.l.; Istituto Superiore di Sanità; Motor Neurone Disease Association
研发日期: October 25 2021
研发阶段: Phase 3
Tauroursodeoxycholic acid (TUDCA) is the taurine conjugate of ursodeoxycholic acid (UDCA) and acts as a mitochondrial stabilizer and anti-apoptotic agent in several models of neurodegenerative diseases, including AD, Parkinson's diseases (PD), and Huntington's diseases (HD).
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