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: 1616632-77-9

TIC10 (ONC201)

中文名称:2,4,6,7,8,9-六氢-4-[(2-甲基苯基)甲基]-7-苄基咪唑并[1,2-a]吡啶并[3,4-e]嘧啶-5(1H)-酮
CAS号:1616632-77-9
分子式: C24H26N4O 分子量: 386.49
产品形式: free base
研发状态: Withdrawn
研发用途: Glioblastoma
研究机构: Masonic Cancer Center University of Minnesota; University of Minnesota
研发日期: June 28 2024
研发阶段: Phase 2
TIC10 (ONC201) inactivates Akt and ERK to induce TNF-related apoptosis-inducing ligand (TRAIL) through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. Phase 1/2.

CAS: 1616493-44-7

Tucidinostat (Chidamide)

中文名称:西达本胺
CAS号:1616493-44-7
分子式: C22H19FN4O2 分子量: 390.41
产品形式: free base
研发状态: Not yet recruiting
研发用途: HR+/HER2- Advanced Breast Cancer
研究机构: Beijing 302 Hospital
研发日期: November 1 2022
研发阶段: Phase 1
Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.

CAS: 1616392-22-3

Pemrametostat (GSK3326595)

CAS号:1616392-22-3
分子式: C24H32N6O3 分子量: 452.55
产品形式: free base
研发状态: Completed
研发用途: Breast Cancer
研究机构: Ottawa Hospital Research Institute; Ontario Institute for Cancer Research; GlaxoSmithKline; London Regional Cancer Program Canada; Hamilton Health Sciences Corporation
研发日期: June 8 2021
研发阶段: Phase 2
Pemrametostat (GSK3326595, EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.

CAS: 1616385-51-3

Bezuclastinib

中文名称:4,5-二甲基-N-(2-苯基-1H-吡咯罗[2,3-b]吡啶-5-基)-1H-吡嗪-3-羧酰胺
CAS号:1616385-51-3
分子式: C19H17N5O 分子量: 331.37
产品形式: free base
研发状态: Not yet recruiting
研发用途: Gastrointestinal Stromal Tumors; GIST
研究机构: Sarcoma Alliance for Research through Collaboration; Cogent Biosciences Inc.; Dana-Farber Cancer Institute; The Life Raft Group
研发日期: Mar-24
研发阶段: Phase 2
Bezuclastinib(CGT9486; PLX 9486) is a potent inhibitor of c-kit and c-kit D816V with an IC50 value of <1 μM. Bezuclastinib is also an inhibitor of tyrosine kinase.

CAS: 1613200-51-3

Tuvusertib

CAS号:1613200-51-3
分子式: C16H12F2N8O 分子量: 370.32
产品形式: free base
研发状态: Not yet recruiting
研发用途: Solid Tumor
研究机构: Institut Curie; ProLynx LLC; Merck Sharp & Dohme LLC
研发日期: June 15 2024
研发阶段: Phase 1
Tuvusertib (M1774, ATR inhibitor 1) is a potent ATR inhibitor, which exhibits anti-proliferative and anti-tumor effects in cancer cell lines.

CAS: 1613191-99-3

VX-803 (M4344)

中文名称:2-氨基-6-氟-N-(5-氟-4-(4-(4-(噁丁环烷-3-基)哌嗪-1-羰基)哌啶-1-基)吡啶-3-基)吡唑并[1,5-A]嘧啶-3-甲酰胺
CAS号:1613191-99-3
分子式: C25H29F2N9O3 分子量: 541.55
产品形式: free base
研发状态: Withdrawn
研发用途: Ovarian Cancer Recurrent
研究机构: University of Alabama at Birmingham
研发日期: May-23
研发阶段: Phase 1
VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. VX-803 (M4344) exhibits potential antineoplastic activity.