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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].

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| Description | 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]. |
| In vitro | Abemaciclib metabolite M18 hydrochloride demonstrates a plasma half-life (T 1/2) of 43.1 hours in healthy subjects [3]. While the primary function of CDK4/6 inhibitors is to prevent retinoblastoma (RB) protein phosphorylation, leading to cell cycle arrest, they also modify cancer cell biology through additional mechanisms [4]. |
| In vivo | CDK4/6 inhibitors enhance T-cell persistence and boost immunological memory in mice administered with tumor-specific CD8+ T cells [5]. |
| Synonyms | LSN3106729 |
| Molecular Weight | 494.54 |
| Formula | C25H28F2N8O |
| Cas No. | 2704316-81-2 |
| Smiles | C(C)(C)N1C=2C(N=C1CO)=C(F)C=C(C2)C3=NC(NC4=CC=C(CN5CCNCC5)C=N4)=NC=C3F |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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