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: 934493-76-2

Voxtalisib (XL765)

中文名称:2-氨基-8-乙基-4-甲基-6-(1H-吡唑-5-基)吡啶并[2,3-d]嘧啶-7(8h)-酮
CAS号:934493-76-2
分子式: C13H14N6O 分子量: 270.29
产品形式: free base
研发状态: Completed
研发用途: Neoplasm Malignant
研究机构: Sanofi
研发日期: Jun-12
研发阶段: Phase 1
Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.

CAS: 934353-76-1

ENMD-2076

中文名称:6-(4-甲基-1-哌嗪基)-N-(5-甲基-1H-吡唑-3-基)-2-[(1E)-2-苯乙烯基]-4-嘧啶胺
CAS号:934353-76-1
分子式: C21H25N7 分子量: 375.47
产品形式: Tartaric Acid
研发状态: Completed
研发用途: Relapsed or Refractory Hematological Malignancies
研究机构: CASI Pharmaceuticals Inc.
研发日期: Apr-09
研发阶段: Phase 1
ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.

CAS: 934343-74-5

HSP990 (NVP-HSP990)

中文名称:(R)-2-氨基-7-[4-氟-2-(6-甲氧基吡啶-2-基)苯基]-4-甲基-7,8-二氢-6H-吡啶并[4,3-d]嘧啶-5-酮
CAS号:934343-74-5
分子式: C20H18FN5O2 分子量: 379.39
产品形式: free base
研发状态: Completed
研发用途: Advanced Solid Malignancies
研究机构: Novartis Pharmaceuticals; Novartis
研发日期: May-09
研发阶段: Phase 1
HSP990 (NVP-HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM. NVP-HSP990 induces cell cycle arrest and apoptosis.

CAS: 93413-69-5

Venlafaxine

中文名称:D,L-文拉法辛
CAS号:93413-69-5
分子式: C17H27NO2 分子量: 277.40
产品形式: Phenethylamine
研发状态: Recruiting
研发用途: Major Depressive Disorder; Bipolar Affective Disorder Currently Depressed Moderate
研究机构: Fondazione IRCCS Ca'' Granda Ospedale Maggiore Policlinico
研发日期: March 1 2022
研发阶段: Phase 4
Venlafaxine (Wy 45030) is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia.

CAS: 93413-62-8

Desvenlafaxine

中文名称: O-去甲文拉法辛
CAS号:93413-62-8
分子式: C16H25NO2 分子量: 263.38
产品形式: Free Base
研发状态: Completed
研发用途: Healthy Subjects
研究机构: Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.; Pfizer
研发日期: Dec-15
研发阶段: Phase 1
Desvenlafaxine (WY 45233 Succinate) is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively.

CAS: 932-30-9

2-Hydroxybenzylamine

中文名称:2-羟基苄胺
CAS号:932-30-9
分子式: C7H9NO 分子量: 123.15
产品形式: Free Base
研发状态: Recruiting
研发用途: Familial Hypercholesterolemia
研究机构: Vanderbilt University Medical Center; National Heart Lung and Blood Institute (NHLBI)
研发日期: February 14 2024
研发阶段: Phase 2
2-Hydroxybenzylamine (2-(Aminomethyl)phenol, 2-HOBA, NSC 127870) is a naturally occurring compound found in buckwheat and is a selective scavenger of dicarbonyl electrophiles that protects proteins and lipids from being modified by these electrophiles. 2-HOBA reduces inflammation and plaque apoptotic cells and promotes efferocytosis and features of stable plaques. 2-HOBA has potential for use as a nutrition supplement due to its ability to protect against the damaging effects of oxidative stress.