| Identification | Back Directory | [Name]
1H-Benzimidazole-2-methanol, 4-fluoro-6-[5-fluoro-2-[[5-(1-piperazinylmethyl)-2-pyridinyl]amino]-4-pyrimidinyl]-1-(1-methylethyl)- | [CAS]
2704316-81-2 | [Synonyms]
2H8]-Abemaciclib metabolite M18 hydrobromide
1H-Benzimidazole-2-methanol, 4-fluoro-6-[5-fluoro-2-[[5-(1-piperazinylmethyl)-2-pyridinyl]amino]-4-pyrimidinyl]-1-(1-methylethyl)- | [Molecular Formula]
C25H28F2N8O | [MOL File]
2704316-81-2.mol | [Molecular Weight]
494.54 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
CDK4/6 inhibitors results T-cell persistence and immunologic memory increasing in mice receiving tumor-specific CD8+ T cells[5].
| [IC 50]
CDK4; CDK6 | [References]
[1] 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.
[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] Palaniappan, et al. Abstract CT153: Pharmacokinetic drug interactions between abemaciclib and CYP3A inducers and inhibitors. Cancer Res. 2016-7-15; 76 (14_Supplement): CT153.
[4] Goel S, et al. CDK4/6 Inhibition in Cancer: Beyond Cell Cycle Arrest. Trends Cell Biol. 2018 Nov;28(11):911-925. DOI:10.1016/j.tcb.2018.07.002
[5] Heckler M, et al. Inhibition of CDK4/6 Promotes CD8 T-cell Memory Formation. Cancer Discov. 2021 Oct;11(10):2564-2581. DOI:10.1158/2159-8290.CD-20-1540 |
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