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: 2097132-94-8

Pralsetinib (BLU-667)

中文名称:BLU-667(拉西替尼)
CAS号:2097132-94-8
分子式: C27H32FN9O2 分子量: 533.60
产品形式: Free base
研发状态: Withdrawn
研发用途: Medullary Thyroid Cancer
研究机构: Hoffmann-La Roche
研发日期: November 30 2023
研发阶段: Phase 3
Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly potent and selective RET (c-RET) inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T).

CAS: 2097002-61-2

Selitrectinib (LOXO-195)

中文名称:赛利替尼
CAS号:2097002-61-2
分子式: C20H21FN6O 分子量: 380.42
产品形式: Free base
研发状态: Completed
研发用途: Solid Tumors Harboring NTRK Fusion
研究机构: Bayer
研发日期: February 28 2020
研发阶段: Phase 1
Selitrectinib (LOXO-195, BAY 2731954) is an orally available, highly potent, and selective TRK kinase inhibitor with low nanomolar inhibitory activity against TRKA G595R, TRKC G623R, and TRKA G667C, IC50s ranging from 2.0 to 9.8 nmol/L. It is more than 1,000-fold selective for 98% of non-TRK kinases tested.

CAS: 2095719-92-7

ASTX-029

CAS号:2095719-92-7
分子式: C29H31ClFN5O5 分子量: 584.04
产品形式: Free base
研发状态: Active not recruiting
研发用途: Solid Tumor Adult
研究机构: Astex Pharmaceuticals Inc.
研发日期: May 10 2018
研发阶段: Phase 1 : Phase 2
ASTX-029 is an orally bioavailable inhibitor of the extracellular signal-regulated kinases (ERK) 1 and 2, with potential antineoplastic activity. ASTX-029 inhibits ERK-dependent tumor cell proliferation and survival.

CAS: 2095432-65-6

Verubecestat (MK-8931) Trifluoroacetate

中文名称:(R)-5-氟-N-(4-氟-3-(3-亚胺基-2,5-二甲基-1,1-二氧化铄-1,2,4-噻二氮-5-基)苯)皮考林酰胺 2,2,2-三氟乙酸酯
CAS号:2095432-65-6
分子式: C19H18F5N5O5S 分子量: 523.43
产品形式: Trifluoroacetat
研发状态: Completed
研发用途: Amnestic Mild Cognitive Impairment; Alzheimer''s Disease; Prodromal Alzheimer''s Disease
研究机构: Merck Sharp & Dohme LLC
研发日期: October 11 2016
研发阶段: Phase 1
Verubecestat (MK-8931) Trifluoroacetate is a potent and selective beta-secretase inhibitor and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor.

CAS: 2095393-15-8

Nemtabrutinib (ARQ 531)

CAS号:2095393-15-8
分子式: C25H23ClN4O4 分子量: 478.93
产品形式: free base
研发状态: Active not recruiting
研发用途: Mature B-cell Neoplasms
研究机构: Merck Sharp & Dohme LLC
研发日期: February 13 2023
研发阶段: Phase 1
Nemtabrutinib (ARQ 531, MK-1026) is an ATP-competitive tyrosine kinase inhibitor designed to target BTK with an IC50 of 0.85 nM. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases.

CAS: 209410-46-8

Neflamapimod (VX-745)

中文名称:5-(2,6-二氯苯基)-2-((2,4-二氟苯基)硫基)-6H-嘧啶并[1,6-b]哒嗪-6-酮
CAS号:209410-46-8
分子式: C19H9Cl2F2N3OS 分子量: 436.26
产品形式: free base
研发状态: Completed
研发用途: Alzheimer''s Disease
研究机构: EIP Pharma Inc
研发日期: Apr-15
研发阶段: Phase 2
Neflamapimod (VX-745) is a potent and selective inhibitor of p38α with IC50 of 10 nM, 22-fold greater selectivity versus p38β and no inhibition to p38γ.