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: 869886-67-9

Ulixertinib (BVD-523)

中文名称: 优立替尼
CAS号:869886-67-9
分子式: C21H22Cl2N4O2 分子量: 433.33
产品形式: free base
研发状态: Terminated
研发用途: Advanced Solid Tumor; BRAF Gene Mutation; BRAF Gene Alteration; MEK Mutation; MEK Alteration; MAP2K1 Gene Mutation; MAP2K1 Gene Alteration; MAP2K2 Gene Mutation; MAP2K2 Gene Alteration
研究机构: BioMed Valley Discoveries Inc
研发日期: November 3 2020
研发阶段: Phase 2
Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

CAS: 869363-13-3

MLN8054

中文名称:4-[[9-氯-7-(2,6-二氟苯基)-5H-嘧啶并[5,4-d][2]苯并氮杂卓-2-基]氨基]苯甲酸
CAS号:869363-13-3
分子式: C25H15ClF2N4O2 分子量: 476.86
产品形式: free base
研发状态: Terminated
研发用途: Advanced Malignancies
研究机构: Millennium Pharmaceuticals Inc.
研发日期: Apr-06
研发阶段: Phase 1
MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1.

CAS: 869357-68-6

AZD8330

中文名称:2-(2-氟-4-碘苯氨基)-N-(2-羟基乙氧基)-1,5-二甲基-6-氧代-1,6-二氢吡啶-3-甲酰胺
CAS号:869357-68-6
分子式: C16H17FIN3O4 分子量: 461.23
产品形式: free base
研发状态: Completed
研发用途: Cancer
研究机构: AstraZeneca
研发日期: Mar-07
研发阶段: Phase 1
AZD8330 (ARRY704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM. Phase 1.

CAS: 868540-17-4

Carfilzomib (PR-171)

中文名称:卡非佐米
CAS号:868540-17-4
分子式: C40H57N5O7 分子量: 719.91
产品形式: free base
研发状态: Recruiting
研发用途: Relapsed or Refractory Multiple Myeloma
研究机构: Bristol-Myers Squibb
研发日期: January 10 2023
研发阶段: Phase 3
Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.

CAS: 868049-49-4

Olodaterol (BI 1744)

中文名称:6-羟基-8-[(1R)-1-羟基-2-[[2-(4-甲氧基苯基)-1,1-二甲基乙基]氨基]乙基]-2H-1,4-苯并恶嗪-3(4H)-酮
CAS号:868049-49-4
分子式: C21H26N2O5 分子量: 386.44
产品形式: Free Base
研发状态: Completed
研发用途: Pulmonary Disease Chronic Obstructive
研究机构: Boehringer Ingelheim; RTI health solutions US
研发日期: February 8 2017
研发阶段: --
Olodaterol (BI 1744) is a long-acting β2-adrenergic receptor agonist that is used as a component of an inhalation (Tiotropium/Olodaterol) for treating patients with chronic obstructive pulmonary disease (COPD).

CAS: 867160-71-2

Linsitinib (OSI-906)

CAS号:867160-71-2
分子式: C26H23N5O 分子量: 421.49
产品形式: free base
研发状态: Completed
研发用途: Relapsed Ewing Sarcoma; Refractory Ewing Sarcoma
研究机构: University of Oxford; European Organisation for Research and Treatment of Cancer - EORTC; European Commission; Astellas Pharma Inc; Oxford University Hospitals NHS Trust
研发日期: Mar-14
研发阶段: Phase 2
Linsitinib (OSI-906) is a selective inhibitor of IGF-1R with IC50 of 35 nM in cell-free assays; modestly potent to InsR with IC50 of 75 nM, and no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3.