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: 75706-12-6

Leflunomide (HWA486)

中文名称:来氟米特
CAS号:75706-12-6
分子式: C12H9F3N2O2 分子量: 270.21
产品形式: free base
研发状态: Recruiting
研发用途: MEN1 Gene Mutation
研究机构: University Hospital Basel Switzerland
研发日期: May 2 2023
研发阶段: Not Applicable
Leflunomide (HWA486, RS-34821, SU101, Arava) is a pyrimidine synthesis and protein tyrosine kinase inhibitor belonging to the DMARD, used as an immunosuppressant agent. The active metabolite of Leflunomide is A77 1726, which inhibits dihydroorotate dehydrogenase (DHODH). Leflunomide is also an agonist of the AhR.

CAS: 75695-93-1

Isradipine

中文名称:伊拉地平
CAS号:75695-93-1
分子式: C19H21N3O5 分子量: 371.39
产品形式: free base
研发状态: Completed
研发用途: Parkinson''s Disease
研究机构: Northwestern University; Northwestern Memorial Hospital
研发日期: Apr-08
研发阶段: Phase 2
Isradipine (PN 200-110) is a potent and selective L-type voltage-gated calcium channel blocker, used to treat high blood pressure.

CAS: 75607-67-9

Fludarabine Phosphate

中文名称:磷酸氟达拉滨
CAS号:75607-67-9
分子式: C10H13FN5O7P 分子量: 365.21
产品形式: Phosphate
研发状态: Not yet recruiting
研发用途: CholangiocarcinomaAdult
研究机构: 3D Medicines (Beijing) Co. Ltd.; 3D Medicines
研发日期: Dec-24
研发阶段: Phase 2
Fludarabine Phosphate (F-ara-A, NSC 312887) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.

CAS: 755038-65-4

Volasertib (BI 6727)

中文名称:伏拉塞替
CAS号:755038-65-4
分子式: C34H50N8O3 分子量: 618.81
产品形式: free base
研发状态: Withdrawn
研发用途: Leukemia Myeloid Acute
研究机构: Boehringer Ingelheim
研发日期: Nov-16
研发阶段: Phase 1
Volasertib (BI 6727) is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Volasertib induces cell cycle arrest and apoptosis in various cancer cells. Phase 3.

CAS: 755038-02-9

BI 2536

中文名称:4-[[(7R)-8-环戊基-7-乙基-5,6,7,8-四氢-5-甲基-6-氧代-2-喋啶基]氨基]-3-甲氧基-N-(1-甲基-4-哌啶基)苯甲酰胺
CAS号:755038-02-9
分子式: C28H39N7O3 分子量: 521.66
产品形式: free base
研发状态: Terminated
研发用途: Pancreatic Neoplasms
研究机构: Boehringer Ingelheim
研发日期: Jun-07
研发阶段: Phase 1
BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.

CAS: 755037-03-7

Regorafenib (BAY 73-4506)

中文名称:瑞格非尼
CAS号:755037-03-7
分子式: C21H15ClF4N4O3 分子量: 482.82
产品形式: free base
研发状态: Not yet recruiting
研发用途: Advanced Gastrointestinal Stromal Tumor
研究机构: Bayer
研发日期: March 20 2024
研发阶段: --
Regorafenib (BAY 73-4506,Fluoro-Sorafenib, Resihance, Stivarga) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy.