Divarasib(GDC-6036,AbMole,M11442)是新一代的KRAS共价抑制剂,Divarasib(CAS No.:2417987-45-0)依赖其亲电性基团(如丙烯酰胺)与KRASG12C蛋白中突变的Cys12形成不可逆的共价加合物,实现对KRASG12C的持久抑制。Divarasib不仅具有持续且显著的共价结合能力,还包含较强的非共价结合成分。Divarasib 在非小细胞肺癌小鼠抑制模型中,10-100 mg/kg的剂量有效抑制了肿瘤的生长。
参考文献
Yadav, V.; Kashif, M.; Kamalia, Z.; et al. Identification of KRAS mutants (G12C, G12D, and G12V) inhibitors. Future medicinal chemistry 2025, 17 (18), 2221-2234.
特别声明:以上内容(如有图片或视频亦包括在内)为自媒体平台“网易号”用户上传并发布,本平台仅提供信息存储服务。
Notice: The content above (including the pictures and videos if any) is uploaded and posted by a user of NetEase Hao, which is a social media platform and only provides information storage services.