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: 923032-37-5

Refametinib (RDEA119)

中文名称:瑞法替尼
CAS号:923032-37-5
分子式: C19H20F3IN2O5S 分子量: 572.34
产品形式: free base
研发状态: Completed
研发用途: Neoplasms
研究机构: Bayer
研发日期: Jul-11
研发阶段: Phase 1
Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.

CAS: 920113-03-7

Riviciclib hydrochloride (P276-00)

中文名称:P276-00抑制剂
CAS号:920113-03-7
分子式: C21H20ClNO5.HCl 分子量: 438.30
产品形式: hydrochloride
研发状态: Completed
研发用途: Squamous Cell Carcinoma of Head and Neck
研究机构: Piramal Enterprises Limited
研发日期: Aug-09
研发阶段: Phase 1 : Phase 2
Riviciclib hydrochloride (P276-00) is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Riviciclib hydrochloride (P276-00) induces apoptosis. Phase 2/3.

CAS: 919783-22-5

AZD1656

CAS号:919783-22-5
分子式: C24H26N6O5 分子量: 478.50
产品形式: free base
研发状态: Completed
研发用途: Type 2 Diabetes Mellitus
研究机构: AstraZeneca
研发日期: Oct-10
研发阶段: Phase 1
AZD1656 is a potent, selective and orally active activator of glucokinase. AZD1656 has the potential for type 2 diabetes research.

CAS: 918633-87-1

Evofosfamide (TH-302)

中文名称: 艾伏磷酰胺
CAS号:918633-87-1
分子式: C9H16Br2N5O4P 分子量: 449.04
产品形式: free base
研发状态: Unknown status
研发用途: Solid Tumors
研究机构: Threshold Pharmaceuticals
研发日期: Nov-13
研发阶段: Phase 1
Evofosfamide (TH-302) is a selective hypoxia-activated prodrug targeting hypoxic regions of solid tumors with IC50 of 19 nM, demonstrates 270-fold enhanced cytotoxicity under hypoxia versus their potency under aerobic conditions, stable to cytochrome P450 metabolism.

CAS: 918504-65-1

Vemurafenib (PLX4032)

中文名称:维罗非尼
CAS号:918504-65-1
分子式: C23H18ClF2N3O3S 分子量: 489.92
产品形式: free base
研发状态: Recruiting
研发用途: Solid Tumor; Haematological Malignancy; Melanoma; Thyroid Cancer Papillary; Ovarian Neoplasms; Colorectal Neoplasms; Laryngeal Neoplasms; Carcinoma Non-Small-Cell Lung; Glioma; Multiple Myeloma; Erdheim-Chester Disease; Thyroid Carcinoma Anaplastic
研究机构: Cancer Research UK; University of Manchester; University of Birmingham; Royal Marsden NHS Foundation Trust; Hoffmann-La Roche
研发日期: March 1 2023
研发阶段: Phase 2 : Phase 3
Vemurafenib (PLX4032, RG7204, RO5185426) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.

CAS: 917879-39-1

MK-2461

中文名称:N-[(2R)-1,4-二恶烷-2-基甲基]-N-甲基-N'-[3-(1-甲基-1H-吡唑-4-基)-5-氧代-5H-苯并[4,5]环庚并[1,2-b]吡啶-7-基]硫酸二酰胺
CAS号:917879-39-1
分子式: C24H25N5O5S 分子量: 495.55
产品形式: free base
研发状态: Completed
研发用途: Neoplasm
研究机构: Merck Sharp & Dohme LLC
研发日期: Jun-07
研发阶段: Phase 1 : Phase 2
MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2.