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: 1644545-52-7

Vorasidenib (AG-881)

中文名称:PVM/MA共聚物
CAS号:1644545-52-7
分子式: C14H13ClF6N6 分子量: 414.74
产品形式: free base
研发状态: Not yet recruiting
研发用途: Low Grade Glioma of Brain
研究机构: Katy Peters MD PhD; Servier; Duke University
研发日期: Jun-24
研发阶段: Phase 1
Vorasidenib (AG-881) is an orally available inhibitor of mutated forms of both isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2).

CAS: 1643913-93-2

KPT 9274 ( ATG-019)

中文名称:(2E)-3-(6-氨基-3-吡啶基)-N-[[5-[4-[(4,4-二氟-1-哌啶基)羰基]苯基]-7-(4-氟苯基)-2-苯并呋喃基]甲基]-2-丙烯酰胺
CAS号:1643913-93-2
分子式: C35H29F3N4O3 分子量: 610.62
产品形式: free base
研发状态: Terminated
研发用途: Solid Tumors; NHL
研究机构: Karyopharm Therapeutics Inc
研发日期: Jun-16
研发阶段: Phase 1
KPT 9274 ( ATG-019) is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay.

CAS: 1643368-58-4

BMS-986142

CAS号:1643368-58-4
分子式: C32H30F2N4O4 分子量: 572.60
产品形式: free base
研发状态: Completed
研发用途: Rheumatoid Arthritis
研究机构: Bristol-Myers Squibb
研发日期: February 16 2016
研发阶段: Phase 2
BMS-986142 is a potent and highly selective reversible small molecule inhibitor of BTK with an IC50 of 0.5 nM. In a panel of 384 kinases, only five kinases were inhibited by BMS-986142 with less than 100-fold selectivity for BTK (TEC, ITK, BLK, TXK and BMX).

CAS: 1642300-52-4

Eltanexor (KPT-8602)

中文名称:艾他尼索
CAS号:1642300-52-4
分子式: C17H10F6N6O 分子量: 428.29
产品形式: free base
研发状态: Recruiting
研发用途: Myelodysplastic Syndromes
研究机构: National Cancer Institute (NCI); National Institutes of Health Clinical Center (CC)
研发日期: November 14 2023
研发阶段: Phase 1 : Phase 2
Eltanexor (KPT-8602, ONO-7706，ATG-016) is a second-generation, orally bioavailable XPO1 (also known as CRM1) inhibitor with IC50 values of 20−211 nM in 10 AML lines after 3 days exposure.

CAS: 1640294-30-9

ASP4132

CAS号:1640294-30-9
分子式: C46H51F3N6O8S2 分子量: 937.06
产品形式: Free Base
研发状态: Completed
研发用途: Lymphoma; Refractory Solid Tumors; Advanced Cancer
研究机构: Astellas Pharma Global Development Inc.; Astellas Pharma Inc
研发日期: March 23 2015
研发阶段: Phase 1
ASP4132 is a potent and orally active activator of Adenosine Monophosphate-Activated Protein Kinase (AMPK) with EC50 of 0.018 μM. ASP4132 is used as a clinical candidate for the treatment of human cancer.

CAS: 1639417-53-0

Tenalisib (RP6530)

中文名称:泰那利塞
CAS号:1639417-53-0
分子式: C23H18FN5O2 分子量: 415.42
产品形式: free base
研发状态: Recruiting
研发用途: Triple Negative Breast Cancer (TNBC)
研究机构: Rhizen Pharmaceuticals SA; Incozen Therapeutics Pvt Ltd
研发日期: March 4 2024
研发阶段: Phase 2
Tenalisib (RP6530) is a potent and selective dual PI3Kδ/γ inhibitor with IC50 values of 24.5 nM and 33.2 nM for PI3Kδ and PI3Kγ, respectively. Its selectivity over α and β isoforms are more than 300-fold and 100-fold, respectively.