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Abemaciclib metabolite M18

Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib , is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader.

Cat. No.: EX-A15152    Purity: >98%
Chemical
Chemical structure of Abemaciclib metabolite M18


For research only, Do not use for Human!

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SynonymsLSN3106729
CAS No.2704316-81-2
Purity>98%
FormulaC25H28F2N8O
Mol Weight494.5396
ColorOff-white to light yellow
StateSolid
Solubilitysoluble in DMSO
Shelf Life>3 years if stored properly
StoragePowder -20℃, 3 years; 4℃, 2 years; In solvent -20℃, 1 month;
ShippingShipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
 
 
Reference:  

[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.

[5]. Heckler M, et al. Inhibition of CDK4/6 Promotes CD8 T-cell Memory Formation. Cancer Discov. 2021 Oct;11(10):2564-2581.

CoACoA of Abemaciclib metabolite M18
Smiles:FC(C=N1)=C(C2=CC(N(C(C)C)C(CO)=N3)=C3C(F)=C2)N=C1NC4=NC=C(C=C4)CN5CCNCC5

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