Monzosertib(Monzosertib) - 药物靶点：CDC7_在研适应症：实体瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

CDC7

作用机制

CDC7抑制剂(细胞分裂周期7相关蛋白激酶抑制剂)

治疗领域

肿瘤

在研适应症

实体瘤

非在研适应症-

原研机构

Carna Biosciences, Inc.

在研机构

Carna Biosciences, Inc.

非在研机构-

最高研发阶段临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C21H22F3N5O4

InChIKeyDNTVXDZWVOVLOD-UHFFFAOYSA-N

CAS号1402057-88-8

关联

1

项与 Monzosertib 相关的临床试验

JPRN-jRCT2031210072 / Recruiting临床1期IIT

An open-label phase I study of AS-0141 in patients with advanced, metastatic, relapsed or refractory malignancies

开始日期2021-06-11

申办/合作机构-

100 项与 Monzosertib 相关的临床结果

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100 项与 Monzosertib 相关的转化医学

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100 项与 Monzosertib 相关的专利（医药）

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1

项与 Monzosertib 相关的文献（医药）

2021-10-14·Journal of Medicinal Chemistry1区 · 医学

Discovery of AS-0141, a Potent and Selective Inhibitor of CDC7 Kinase for the Treatment of Solid Cancers

1区 · 医学

Article

作者: Masai, Hisao ; Sawa, Masaaki ; Funakoshi, Yoko ; Taniyama, Chika ; Irie, Takayuki ; Asami, Tokiko ; Uno, Yuko ; Sawa, Ayako

CDC7, a serine-threonine kinase, plays conserved and important roles in regulation of DNA replication and has been recognized as a potential anticancer target. We report here the optimization of a series of furanone analogues starting from compound 1 with a focus on ADME properties suitable for clinical development. By replacing the 2-chlorobenzene moiety in 1 with various aliphatic groups, we identified compound 24 as a potent CDC7 inhibitor with excellent kinase selectivity and favorable oral bioavailability in multiple species. Oral administration of 24 demonstrated robust in vivo antitumor efficacy in a colorectal cancer xenograft model. Compound 24 (AS-0141) is currently in phase I clinical trials for the treatment of solid cancers.

100 项与 Monzosertib 相关的药物交易

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