YF-PRJ8-1011(YF-PRJ8-1011) - 药物靶点：CDK4 x CDK6_在研适应症：胶质瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

CDK4 x CDK6

作用机制

CDK4抑制剂(细胞周期蛋白依赖性激酶4抑制剂)、CDK6抑制剂(细胞周期蛋白依赖性激酶6抑制剂)

治疗领域

肿瘤神经系统疾病

在研适应症

胶质瘤

非在研适应症-

原研机构

珠海宇繁生物科技有限责任公司

在研机构

珠海宇繁生物科技有限责任公司

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C24H29FN8O

InChIKeyUHLNOIFXSTUOIQ-UHFFFAOYSA-N

CAS号2497593-03-8

关联

100 项与 YF-PRJ8-1011 相关的临床结果

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100 项与 YF-PRJ8-1011 相关的转化医学

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100 项与 YF-PRJ8-1011 相关的专利（医药）

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1

项与 YF-PRJ8-1011 相关的文献（医药）

2023-05-01·Journal of neuro-oncology

A novel CDK4/6 inhibitor combined with irradiation demonstrates potent anti-tumor efficacy in diffuse midline glioma.

Article

作者: Wu, Zhen ; Zhang, Liwei ; Liao, Xuebin ; Zhang, Junting ; Lin, Xingyu ; Zuo, Pengcheng ; Li, Yaopeng ; Wang, Tantan

Diffuse midline glioma, H3 K27-altered (DMG) is a lethal pediatric brainstem tumor.Despite numerous efforts to improve survival benefits, its prognosis remains poor.This study aimed to design and synthesize a novel CDK4/6 inhibitor YF-PRJ8-1011, which exhibited more potent antitumor activity against a panel of patient-derived DMG tumor cells in vitro and in vivo compared with palbociclib.Patient-derived DMG cells were used to assess the antitumor efficacy of YF-PRJ8-1011 in vitro.The liquid chromatog. tandem-mass spectrometry method was used to measure the activity of YF-PRJ8-1011 passing through the blood-brain barrier.DMG patient-derived xenograft models were established to detect the antitumor efficacy of YF-PRJ8-1011.The results showed that YF-PRJ8-1011 could inhibit the growth of DMG cells both in vitro and in vivo.YF-PRJ8-1011 could well penetrate the blood-brain barrier.It also significantly inhibited the growth of DMG tumors and prolonged the overall survival of mice compared with vehicle or palbociclib.Most notably, it exerted potent antitumor efficacy in DMG in vitro and in vivo compared with palbociclib.In addition, we also found that YF-PRJ8-1011 combined with radiotherapy also showed more significant inhibition of DMG xenograft tumor growth than radiotherapy alone.Collectively, YF-PRJ8-1011 is a novel, safe, and selective CDK4/6 inhibitor for DMG treatment.

100 项与 YF-PRJ8-1011 相关的药物交易

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