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: 2110428-64-1

JNJ-63576253 (TRC-253)

CAS号:2110428-64-1
分子式: C23H22ClF3N6O2S 分子量: 538.97
产品形式: Free Base
研发状态: Completed
研发用途: Metastatic Castrate-resistant Prostate Cancer; Adenocarcinoma Prostate
研究机构: Tracon Pharmaceuticals Inc.; Janssen Pharmaceutica N.V. Belgium
研发日期: May 23 2017
研发阶段: Phase 1 : Phase 2
JNJ-63576253 (TRC-253) is a potent and selective androgen receptor (AR) Antagonist with IC50 of 6.9 nM. JNJ-63576253 displays robust inhibition in WT and LBD-mutated, enzalutamide-resistant models of prostate cancer.

CAS: 2105904-82-1

AB680

CAS号:2105904-82-1
分子式: C20H24ClFN4O9P2 分子量: 580.82
产品形式: chloride ; hydrogen phosphite
研发状态: Completed
研发用途: Healthy Volunteers
研究机构: Arcus Biosciences Inc.
研发日期: October 20 2020
研发阶段: Phase 1
AB-680 is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73.

CAS: 2101700-15-4

Pirtobrutinib (LOXO-305)

中文名称:5-氨基-3-[4-[(5-氟-2-甲氧基苯甲酰基)氨基]甲基]苯基]-1-[(1S)-2,2,2-三氟-1-甲基乙基]-1H-吡唑-4-甲酰胺
CAS号:2101700-15-4
分子式: C22H21F4N5O3 分子量: 479.43
产品形式: Free base
研发状态: Withdrawn
研发用途: Relapsing Multiple Sclerosis; Multiple Sclerosis
研究机构: Loxo Oncology Inc.; Eli Lilly and Company
研发日期: May 1 2024
研发阶段: Phase 2
Pirtobrutinib (LOXO-305, LY 3527727, RXC-005) is a highly selective, non-covalent, next generation BTK inhibitor with an IC50 of 5.69 nM in WT BTK HEK cells. Pirtobrutinib shows more than 300-fold selective for BTK over 98% of 370 other kinases.

CAS: 209860-87-7

Tafluprost

中文名称: 他氟前列素
CAS号:209860-87-7
分子式: C25H34F2O5 分子量: 452.53
产品形式: Prostaglandin analogue
研发状态: Completed
研发用途: Ocular Surface Disease; Primary Open Angle Glaucoma
研究机构: Santen Pharmaceutical (Taiwan) Co. LTD
研发日期: September 1 2021
研发阶段: --
Tafluprost (AFP-168,MK2452) is a novel prostaglandin analog with a high affinity for the fluoroprostaglandin (FP) receptor PGF2α. A prostanoid selective FP receptor agonist.

CAS: 2097938-73-1

MBQ-167

CAS号:2097938-73-1
分子式: C22H18N4 分子量: 338.41
产品形式: Free Base
研发状态: Recruiting
研发用途: Breast Cancer; Breast Neoplasm; Breast Cancer Stage IV
研究机构: MBQ Pharma; Congressionally Directed Medical Research Programs
研发日期: November 9 2023
研发阶段: Phase 1
MBQ-167 is a potent and dual inhibitor of Rac and Cdc42 with IC50s of 103 nM and 78 nM respectively, in metastatic breast cancer cells.

CAS: 209783-80-2

Entinostat (MS-275)

中文名称:恩替诺特
CAS号:209783-80-2
分子式: C21H20N4O3 分子量: 376.41
产品形式: free base
研发状态: Recruiting
研发用途: Oropharyngeal Cancer; Neck Cancer; Human Papillomavirus; HPV; Anal Cancer; Cervical Cancer; Penile Cancer; Vulvar Cancer; Vaginal Cancer; Colon Cancer
研究机构: National Cancer Institute (NCI); National Institutes of Health Clinical Center (CC)
研发日期: October 5 2021
研发阶段: Phase 1 : Phase 2
Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3.