Abemaciclib metabolite M18-d8(Synonyms: LSN3106729-d8)

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Abemaciclib metabolite M18-d8 (Synonyms: LSN3106729-d8)

Abemaciclib metabolite M18-d8 (LSN3106729-d8) 是 Abemaciclib metabolite M18 的氘代物。Abemaciclib metabolite M18 (LSN3106729),Abemaciclib 的代谢物, 是一种具有抗肿瘤活性的 CDK 抑制剂。Abemaciclib metabolite M18 和 CRBN 配体可用于设计 PROTAC CDK4/6 降解剂。

Abemaciclib metabolite M18-d8(Synonyms: LSN3106729-d8)

Abemaciclib metabolite M18-d8 Chemical Structure

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生物活性

Abemaciclib metabolite M18-d8 (LSN3106729-d8) is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

502.59

Formula

C25H20D8F2N8O

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1.

    [3]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non–Small Cell Lung Cancer: A Phase Ib Study.

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