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Ribociclib succinate (LEE011 succinate) is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth.Responsiveness of neuroblastoma xenografts to LEE011 translated to the in vivo setting in that there was a direct correlation of in vitro IC50 values with degree of subcutaneous xenograft growth delay.
Mol Cancer Ther. 2022 Aug 2;21(8):1306-1317.
Combination of Ribociclib and Gemcitabine for the Treatment of Medulloblastoma.
Ribociclib succinate (LEE011 succinate) purchased from AbMole
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Source | Nature (2018). Figure 2. Ribociclib |
| Method | IB analysis | |
| Cell Lines | 4T1 tumor cell lines | |
| Concentrations | 1 μM | |
| Incubation Time | 36 h | |
| Results | "Furthermore, treatment of multiple cancer cell lines with two different selective inhibitors of CDK4/6 kinase, palbociclib or ribociclib, upregulated PD-L1 protein abundance and stability even in pRB knock-down cells." |
| Molecular Weight | 552.63 |
| Formula | C27H36N8O5 |
| CAS Number | 1374639-75-4 |
| Solubility (25°C) | DMSO ≥ 9 mg/mL Water 3 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50 values of 1.2 and 1.3 nM, respectively. |
| CDK9-IN-1
CDK9-IN-1 is a novel, selective CDK9 inhibitor, with an IC50 of 39 nM for CDK9/CycT1, it can be used for the research of HIV infection. |
| XO44
XO44 (PF-6808472) is a broad-spectrum covalent kinase probe. |
| ML 315
ML 315 is a selective dual inhibitor of CDK and DYRK with IC50s of 68 nM and 282 nM, respectively. |
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