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: 84929-27-1

Grape Seed Extract

中文名称:葡萄籽提取物
CAS号:84929-27-1
分子式: N/A 分子量: N/A
产品形式: Polyphenols
研发状态: Completed
研发用途: Solid Cancers
研究机构: Medical University of South Carolina
研发日期: Mar-13
研发阶段: Phase 1
Grape Seed Extract are industrial derivatives from whole grape seeds that have a great concentration of vitamin E, flavonoids, linoleic acid, and OPCs.

CAS: 849217-68-1

Cabozantinib (BMS-907351)

中文名称:卡博替尼
CAS号:849217-68-1
分子式: C28H24FN3O5 分子量: 501.51
产品形式: Free Base
研发状态: Recruiting
研发用途: Ewing Sarcoma; Osteosarcoma
研究机构: Children''s Hospital of Philadelphia; Children''s Hospital Colorado; Exelixis; Alex''s Lemonade Stand Foundation
研发日期: October 24 2023
研发阶段: Phase 1
Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway.

CAS: 849217-64-7

Foretinib (GSK1363089)

CAS号:849217-64-7
分子式: C34H34F2N4O6 分子量: 632.65
产品形式: free base
研发状态: Completed
研发用途: Carcinoma Hepatocellular
研究机构: GlaxoSmithKline
研发日期: August 12 2009
研发阶段: Phase 1
Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.

CAS: 848942-61-0

Sapitinib (AZD8931)

中文名称:Az08931 2-(4-(4-(3-氯-2-氟苯基氨基)-7-甲氧基喹唑啉-6-基氧基)哌啶-1-基)-n-甲基乙酰胺
CAS号:848942-61-0
分子式: C23H25ClFN5O3 分子量: 473.93
产品形式: free base
研发状态: Terminated
研发用途: Breast Neoplasm
研究机构: AstraZeneca
研发日期: Jun-12
研发阶段: Phase 1
Sapitinib (AZD8931) is a reversible, ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 with IC50 of 4 nM, 3 nM and 4 nM in cell-free assays, more potent than Gefitinib or Lapatinib against NSCLC cell, 100-fold more selective for the ErbB family than MNK1 and Flt. Phase 2.

CAS: 848695-25-0

BIIB021

中文名称:6-氯-9-[(4-甲氧基-3,5-二甲基-2-吡啶基)甲基]-9H-嘌呤-2-胺
CAS号:848695-25-0
分子式: C14H15ClN6O 分子量: 318.76
产品形式: free base
研发状态: Completed
研发用途: Advanced Solid Tumors
研究机构: Biogen
研发日期: Nov-09
研发阶段: Phase 1
BIIB021 (CNF2024) is an orally available, fully synthetic small-molecule inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively. Phase 2.

CAS: 848141-11-7

Alvelestat (AZD9668)

中文名称:6-甲基-5-(1-甲基-1H-吡唑-5-基)-N-((5-甲基磺基)吡啶-2-基)甲基)-2-氧代-1-(3-三氟甲基)苯基)-1,2-二氢吡啶-3-甲酰胺
CAS号:848141-11-7
分子式: C25H22F3N5O4S 分子量: 545.53
产品形式: free base
研发状态: Withdrawn
研发用途: Pharmacokinetics; Pharmacodynamics
研究机构: AstraZeneca
研发日期: Nov-10
研发阶段: Phase 1
Alvelestat (AZD9668, Avelestat) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, at least 600-fold more selective over other serine proteases. Phase 2.