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: 119623-66-4

Diclofenac Epolamine

中文名称:双氯芬酸依泊胺
CAS号:119623-66-4
分子式: C20H24Cl2N2O3 分子量: 411.32
产品形式: Epolamine
研发状态: Completed
研发用途: Breast Cancer
研究机构: Northwestern University
研发日期: Jun-11
研发阶段: Early Phase 1
Diclofenac Epolamine (DHEP, DIEP, diclofenac hydroxyethylpyrrolidine) is a non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions.

CAS: 1195768-06-9

Dabrafenib Mesylate

中文名称: 达帕菲尼甲磺酸盐
CAS号:1195768-06-9
分子式: C23H20F3N5O2S2.CH4O3S 分子量: 615.67
产品形式: mesylate
研发状态: Completed
研发用途: Metastatic Cancer; Melanoma; Colon Cancer; Differentiated Thyroid Cancer; Hepatocellular Carcinoma; Renal Cell Carcinoma; Metastatic Melanoma; HCC; Metastatic Colon Cancer
研究机构: University of Arizona
研发日期: October 17 2014
研发阶段: Not Applicable
Dabrafenib Mesylate (GSK2118436) is the mesylate salt form of dabrafenib, an orally bioavailable inhibitor of B-raf (BRAF) protein with IC50s of 0.8 nM, 3.2 nM and 5 nM for B-Raf (V600E), B-Raf (WT) and C-Raf, respectively.

CAS: 1195765-45-7

Dabrafenib (GSK2118436)

中文名称:达拉菲尼
CAS号:1195765-45-7
分子式: C23H20F3N5O2S2 分子量: 519.56
产品形式: free base
研发状态: Recruiting
研发用途: Anaplastic Thyroid Cancer
研究机构: Leiden University Medical Center; Novartis
研发日期: January 1 2023
研发阶段: Phase 2
Dabrafenib (GSK2118436, GSK2118436A) is a mutant BRAFV600E specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.

CAS: 1194506-26-7

Fruquintinib (HMPL-013)

中文名称:呋喹替尼
CAS号:1194506-26-7
分子式: C21H19N3O5 分子量: 393.39
产品形式: Tyrosine kinase inhibitor
研发状态: Active not recruiting
研发用途: Triple Negative Breast Cancer; Endometrial Cancer; Solid Tumor Unspecified Adult; Colorectal Cancer
研究机构: Hutchison Medipharma Limited; BeiGene; Hutchmed
研发日期: August 9 2021
研发阶段: Phase 1 : Phase 2
Fruquintinib (HMPL-013) is a small molecule inhibitor with strong potency and high selectivity against VEGFR family. It inhibits VEGFR 1, 2, 3, with IC50 values of 33 nM, 35 nM and 0.5 nM, respectively and shows only weak inhibition of RET, FGFR-1 and c-kit kinases.

CAS: 119413-54-6

Topotecan (NSC609699) HCl

中文名称:盐酸拓扑替康
CAS号:119413-54-6
分子式: C23H23N3O5.HCl 分子量: 457.91
产品形式: Hydrochloride
研发状态: Terminated
研发用途: Eye Cancer Retinoblastoma
研究机构: Prof. Beck Popovic Maja; University of Lausanne Hospitals
研发日期: November 15 2021
研发阶段: Phase 2
Topotecan HCl (Nogitecan HCl, SKFS 104864A,Hycamtin, NSC 609699) is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis.

CAS: 1194044-20-6

LY2811376

中文名称:(4S)-4-[2,4-二氟-5-(5-嘧啶)苯基]-5,6-二氢-4-甲基-4H-1,3-噻嗪-2-胺
CAS号:1194044-20-6
分子式: C15H14F2N4S 分子量: 320.36
产品形式: free base
研发状态: Completed
研发用途: Alzheimer''s Disease
研究机构: Eli Lilly and Company
研发日期: Dec-08
研发阶段: Phase 1
LY2811376 is the first orally available non-peptidic β-secretase(BACE1) inhibitor with IC50 of 239 nM-249 nM, that act to decrease Aβ secretion with EC50 of 300 nM, demonstrated to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin. Phase 1.