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临床前CDMO研发化合物筛选
Lumacaftor (VX-809)
中文名称:鲁玛卡托
CAS号:936727-05-8
分子式: C24H18F2N2O5 分子量: 452.41
产品形式: free base
研发状态: Completed
研发用途: Cystic Fibrosis Homozygous for Phe 508 Del CFTR; Glucose Intolerance or Newly Diagnosis Diabetes
研究机构: University Hospital Strasbourg France
研发日期: February 11 2016
研发阶段: --
Lumacaftor (VX-809, VRT 826809) acts to correct CFTR mutations common in cystic fibrosis by increasing mutant CFTR (F508del-CFTR) maturation,EC50 of 0.1 μM in fisher rat thyroid cells. Phase 3.
Sacubitril/valsartan (LCZ696)
CAS号:936623-90-4
分子式: C24H29N5O3.C24H29NO5.5/2H2O.3Na 分子量: 915.98
产品形式: Sodium salt hydrate
研发状态: Recruiting
研发用途: Neoplasms
研究机构: Advanced Accelerator Applications
研发日期: July 24 2019
研发阶段: Phase 1 : Phase 2
Sacubitril/valsartan (LCZ696, Sacubitril, Valsartan), consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.
Ibrutinib (PCI-32765)
中文名称:依鲁替尼
CAS号:936563-96-1
分子式: C25H24N6O2 分子量: 440.50
产品形式: free base
研发状态: Not yet recruiting
研发用途: Chronic Lymphocytic Leukemia
研究机构: Gruppo Italiano Malattie EMatologiche dell''Adulto
研发日期: May-24
研发阶段: --
Ibrutinib (PCI-32765,Imbruvica) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc. Ibrutinib is applicable as a Btk ligand in the synthesis of a series of PROTACs including P13I.
Manogepix (E1210)
CAS号:936339-60-5
分子式: C21H18N4O2 分子量: 358.39
产品形式: Free base
研发状态: Active not recruiting
研发用途: Hepatic Impairment
研究机构: Basilea Pharmaceutica
研发日期: October 31 2022
研发阶段: Phase 1
Manogepix (E1210, MGX, APX001A) is a broad-spectrum and orally active antifungal agent that inhibits Gwt1/Gwt1p (GPI-anchored wall transfer protein 1), a protein that plays an important role in fungal cell wall integrity.
Fedratinib (TG101348)
中文名称:N-(1,1-二甲基乙基)-3-[[5-甲基-2-[[4-[2-(1-吡咯烷基)乙氧基]苯基]氨基]-4-嘧啶基]氨基]苯磺酰胺
CAS号:936091-26-8
分子式: C27H36N6O3S 分子量: 524.68
产品形式: free base
研发状态: Recruiting
研发用途: IDH Mutation; IDH1 Mutation; IDH2 Gene Mutation; Blood Cancer; Myeloproliferative Neoplasm
研究机构: University of Chicago
研发日期: October 29 2021
研发阶段: Phase 1
Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2.
Oprozomib (ONX 0912)
中文名称:Oprozomib(ONX-0912)抑制剂
CAS号:935888-69-0
分子式: C25H32N4O7S 分子量: 532.61
产品形式: free base
研发状态: Terminated
研发用途: Multiple Myeloma
研究机构: Amgen
研发日期: July 30 2014
研发阶段: Phase 1
Oprozomib (ONX 0912, PR-047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2.
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