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: 1225497-78-8

Rigosertib (ON-01910)

CAS号:1225497-78-8
分子式: C21H24NNaO8S 分子量: 473.47
产品形式: Sodium Salt
研发状态: Recruiting
研发用途: Recessive Dystrophic Epidermolysis Bullosa
研究机构: Thomas Jefferson University; Traws Pharma Inc.
研发日期: August 24 2021
研发阶段: Early Phase 1
Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K/Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells. Phase 3.

CAS: 1225037-39-7

Bimiralisib (PQR309)

CAS号:1225037-39-7
分子式: C17H20F3N7O2 分子量: 411.38
产品形式: Free Base
研发状态: Completed
研发用途: Cancer
研究机构: PIQUR Therapeutics AG; Roswell Park Cancer Institute; M.D. Anderson Cancer Center; Mayo Clinic; Hospital Clinic of Barcelona; University College London Hospitals; Churchill Hospital; Case Western Reserve University; University Hospital Zürich
研发日期: March 21 2019
研发阶段: Phase 1
Bimiralisib (PQR309) is a novel brain-penetrant dual PI3K/mTOR inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets.

CAS: 1224887-10-8

GSK2256098

中文名称:2-[[5-氯-2-[[3-甲基-1-(1-甲基乙基)-1H-吡唑-5-基]氨基]-4-吡啶基]氨基]-N-甲氧基苯甲酰胺
CAS号:1224887-10-8
分子式: C20H23ClN6O2 分子量: 414.89
产品形式: free base
研发状态: Completed
研发用途: Hypertension Pulmonary
研究机构: GlaxoSmithKline
研发日期: November 17 2015
研发阶段: Phase 1
GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. GSK2256098 inhibits cancer cell growth and induces apoptosis.

CAS: 1224844-38-5

Sapanisertib (MLN0128)

中文名称:沙帕色替
CAS号:1224844-38-5
分子式: C15H15N7O 分子量: 309.33
产品形式: free base
研发状态: Recruiting
研发用途: Leptomeningeal Neoplasm; Metastatic Lung Non-Small Cell Carcinoma; Metastatic Malignant Neoplasm in the Brain; Recurrent Lung Non-Small Cell Carcinoma; Stage IV Lung Cancer AJCC v8; Stage IVA Lung Cancer AJCC v8; Stage IVB Lung Cancer AJCC v8
研究机构: National Cancer Institute (NCI)
研发日期: October 26 2020
研发阶段: Phase 1
Sapanisertib (MLN0128, INK 128, TAK-228) is a potent and selective mTOR inhibitor with IC50 of 1 nM in cell-free assays; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.

CAS: 1223405-08-0

Larotrectinib (LOXO-101) sulfate

中文名称:硫酸拉罗替尼
CAS号:1223405-08-0
分子式: C21H22F2N6O2.H2SO4 分子量: 526.51
产品形式: sulfate
研发状态: Recruiting
研发用途: High Grade Glioma; Diffuse Intrinsic Pontine Glioma
研究机构: Nationwide Children''s Hospital
研发日期: April 8 2021
研发阶段: Early Phase 1
Larotrectinib sulfate (LOXO-101, ARRY-470) is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). Larotrectinib inhibition of TRKs induces cellular apoptosis and G1 cell-cycle arrest.

CAS: 1223403-58-4

Larotrectinib

中文名称:拉罗替尼
CAS号:1223403-58-4
分子式: C21H22F2N6O2 分子量: 428.44
产品形式: Free Base
研发状态: Recruiting
研发用途: High Grade Glioma; Diffuse Intrinsic Pontine Glioma
研究机构: Nationwide Children''s Hospital
研发日期: April 8 2021
研发阶段: Early Phase 1
Larotrectinib (Vitrakvi, LOXO-101, ARRY-470) is an ATP-competitive, oral administered and highly selective inhibitor of the tropomyosin-related kinase (TRK) family receptors.