临床前CDMO研发筛选相关化合物

CDMO是Contract Development and Manufacturing Organization的缩写，即合同定制研发生产组织。它是一种为制药企业及生物技术公司提供医药（特别是创新药）工艺研发及制备、工艺优化、放大生产、注册和验证批生产以及商业化生产等定制服务的机构. 在传统代工基础上增加了研发和工艺优化能力，是高技术壁垒的工艺研发能力与规模生产能力的深度结合. 1, 工艺开发与优化：创新性合成路线设计、工艺参数优化. 2, 中试放大：实验室工艺向规模化生产的转化 3, 注册批生产：支持客户新药申报的验证批生产. 4, 商业化生产：药品上市后的大规模生产供应. 全球医药CDMO行业保持较高景气度。根据弗若斯特沙利文预测：2026年全球CDMO市场规模：预计达1,189亿美元 2033年全球CDMO市场规模：预计达3,385亿美元. CDMO作为医药产业链专业化分工的产物，已经从单纯的CMO代工模式升级为"研发+生产"一体化的高附加值服务。当前，在多肽、ADC、CGT等新型药物赛道的驱动下，全球及中国CDMO市场保持高速增长。中国CDMO企业凭借完整的供应链体系、工程师红利和一体化服务能力，全球市占率有望持续提升，行业正从"成本优势"竞争迈向"体系优势"竞争的新阶段。
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临床前CDMO研发化合物筛选

CAS: 3424-98-4

Telbivudine

中文名称:替比夫定
CAS号:3424-98-4
分子式: C10H14N2O5 分子量: 242.23
产品形式: free base
研发状态: Completed
研发用途: Hepatitis B Chronic
研究机构: Hoffmann-La Roche
研发日期: December 12 2016
研发阶段: Phase 1
Telbivudine(NV 02B) is a potent, and selective HBV reverse transcriptase inhibitor, used to treat HBV infection.

CAS: 34183-22-7

Propafenone HCl

中文名称: 心律平
CAS号:34183-22-7
分子式: C21H27NO3.HCl 分子量: 377.90
产品形式: Hydrochloride
研发状态: Completed
研发用途: Bioequivalence
研究机构: Pharmtechnology LLC; Altasciences Company Inc.
研发日期: March 23 2019
研发阶段: Phase 1
Propafenone HCl is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias.

CAS: 34157-83-0

Celastrol (NSC 70931)

中文名称:雷公藤红素; 南蛇藤素
CAS号:34157-83-0
分子式: C29H38O4 分子量: 450.61
产品形式: free base
研发状态: Recruiting
研发用途: Safety
研究机构: Legend Labz Inc.
研发日期: May 25 2022
研发阶段: Not Applicable
Celastrol (NSC 70931, Tripterine) is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.

CAS: 341031-54-7

Sunitinib (SU11248) malate

中文名称:苹果酸舒尼替尼
CAS号:341031-54-7
分子式: C22H27FN4O2.C4H6O5 分子量: 532.56
产品形式: Malate
研发状态: Not yet recruiting
研发用途: Carcinoma Renal Cell
研究机构: State University of New York at Buffalo
研发日期: June 1 2024
研发阶段: Phase 1 : Phase 2
Sunitinib (SU11248) malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.

CAS: 34031-32-8

Auranofin

中文名称:金诺芬
CAS号:34031-32-8
分子式: C20H34AuO9PS 分子量: 678.48
产品形式: Free Base
研发状态: Completed
研发用途: Amoebiasis
研究机构: National Institute of Allergy and Infectious Diseases (NIAID)
研发日期: April 2 2014
研发阶段: Phase 1
Auranofin (Ridaura, SKF-39162) is an inhibitor of thioredoxin reductase (TrxR) with IC50 of 88 nM for purified H. pylori TrxR in cell-free assay. Auranofin has anti-cancer activity and can completely inhibit bacterial growth at 1.2 μM. Auranofin is an FDA-approved gold-containing compound used for the treatment of rheumatoid arthritis.

CAS: 336113-53-2

Ispinesib (SB-715992)

中文名称:伊斯平斯
CAS号:336113-53-2
分子式: C30H33ClN4O2 分子量: 517.06
产品形式: free base
研发状态: Terminated
研发用途: Breast Neoplasms
研究机构: Cytokinetics
研发日期: Dec-07
研发阶段: Phase 1
Ispinesib (SB-715992, CK0238273) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP) with Ki app of 1.7 nM in a cell-free assay, no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Ispinesib induces mitotic arrest and apoptotic cell death.