产品描述：

Abemaciclib metabolite M18 (LSN3106729) is a potent cyclin-dependent kinase (CDK) inhibitor with antitumor properties. It has been incorporated alongside a cereblon (CRBN) ligand to develop a proteolysis-targeting chimera (PROTAC) that selectively degrades CDK4/6 [1] [2].

体外活性

In the plasma of healthy subjects, the metabolite M18 hydrochloride of Abemaciclib has a half-life (T1/2) of 43.1 hours [3]. CDK4/6 inhibitors primarily function by inhibiting the phosphorylation of retinoblastoma (RB) protein to induce cell cycle arrest, and they also alter the biological characteristics of cancer cells through other mechanisms [4].

In vivo, CDK4/6 inhibitors can enhance the survival and immunological memory of tumor-specific CD8+ T cells in mice [5].

别名 LSN3106729

分子量 494.54

分子式 C25H28F2N8O

CAS No. 2704316-81-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

PROteolysis TArgeting Chimeras (PROTACs) 通过将靶蛋白和 E3 连接酶结合起来，从而“劫持”细胞的泛素-蛋白酶体系统（UPS）来实现蛋白质的降解。由于 PROTACs 只需具有高选择性地结合其靶标（而不是抑制靶蛋白的酶活性），目前有许多努力将先前无效的抑制剂分子改造为 PROTACs，用作下一代药物。

产地：西安

用途：科研！

厂家：西安齐岳生物科技有限公司

温馨提示：仅用于科研，不能用于人体实验！

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