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: 1032754-93-0

Apitolisib (GDC-0980)

中文名称:(S)-1-[4-[[2-(2-氨基嘧啶-5-基)-7-甲基-4-(吗啉-4-基)噻吩并[3,2-D]嘧啶-6-基]甲基]哌嗪-1-基]-2-羟基丙-1-酮
CAS号:1032754-93-0
分子式: C23H30N8O3S 分子量: 498.60
产品形式: free base
研发状态: Completed
研发用途: Healthy Volunteer
研究机构: Genentech Inc.
研发日期: Dec-11
研发阶段: Phase 1
Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2.

CAS: 1032350-13-2

MK-2206 2HCl

中文名称:8-[4-(1-氨基环丁基)苯基]-9-苯基-1,2,4-噻唑并[3,4-f][1,6]萘啶-3(2H)-酮双盐酸盐
CAS号:1032350-13-2
分子式: C25H21N5O.2HCl 分子量: 480.39
产品形式: Dihydrochloride
研发状态: Active not recruiting
研发用途: Advanced Malignant Solid Neoplasm; Stage III Cutaneous Melanoma AJCC v7; Stage III Prostate Cancer AJCC v7; Stage III Renal Cell Cancer AJCC v7; Stage IIIA Cutaneous Melanoma AJCC v7; Stage IIIB Cutaneous Melanoma AJCC v7; Stage IIIC Cutaneous Melanoma AJCC v7; Stage IV Cutaneous Melanoma AJCC v6 and v7; Stage IV Prostate Cancer AJCC v7; Stage IV Renal Cell Cancer AJCC v7
研究机构: National Cancer Institute (NCI)
研发日期: November 23 2011
研发阶段: Phase 1
MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM in cell-free assays, respectively; no inhibitory activities against 250 other protein kinases observed. MK-2206 2HCl induces autophagy and apoptosis in cancer cells. Phase 2.

CAS: 1032008-74-4

Endoxifen HCl

中文名称:Z-因多昔芬盐酸盐
CAS号:1032008-74-4
分子式: C25H28ClNO2 分子量: 409.95
产品形式: Hydrochloride
研发状态: Recruiting
研发用途: Breast Neoplasms; Invasive Breast Cancer; Estrogen-receptor-positive Breast Cancer; HER2-negative Breast Cancer
研究机构: Atossa Therapeutics Inc.; InClin
研发日期: February 14 2023
研发阶段: Phase 2
Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.

CAS: 103129-82-4

Levamlodipine

中文名称:苯磺酸左旋氨氯地平
CAS号:103129-82-4
分子式: C20H25ClN2O5 分子量: 408.88
产品形式: free base
研发状态: Completed
研发用途: Hypertension
研究机构: Chong Kun Dang Pharmaceutical
研发日期: Feb-15
研发阶段: Phase 1
Levamlodipine (S-amlodipine) is a pharmacologically active enantiomer of amlodipine which belongs to the dihydropyridine group of calcium channel blocker. It acts on the L-type of calcium channels and its treatment results in vasodilation and a fall in blood pressure.

CAS: 103060-53-3

Daptomycin (LY146032)

中文名称:达托霉素
CAS号:103060-53-3
分子式: C72H101N17O26 分子量: 1620.67
产品形式: free base
研发状态: Unknown status
研发用途: Outcome Fatal; Infection
研究机构: Zhongnan Hospital
研发日期: December 1 2020
研发阶段: --
Daptomycin (Cubicin,LY146032) is a novel antibiotic with rapid in vitro bactericidal activity against gram-positive organisms.

CAS: 1029877-94-8

Trelagliptin succinate

中文名称:琥珀酸曲格列汀
CAS号:1029877-94-8
分子式: C18H20FN5O2.C4H6O4 分子量: 475.47
产品形式: succinate
研发状态: Completed
研发用途: Healthy
研究机构: Takeda
研发日期: Mar-15
研发阶段: Phase 1
Trelagliptin succinate (SYR472) is a dipeptidyl peptidase IV (DPP-4) inhibitor which is used as a new long-acting drug for once-weekly treatment of type 2 diabetes mellitus (DM).