| Name | Ribociclib succinate |
| Description | Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and exhibits over 1,000-fold reduced potency against the cyclin B/CDK1 complex. |
| In vitro | Ribociclib succinate treatment of two neuroblastoma cell lines (BE2C and IMR5) with demonstrated sensitivity to CDK4/6 inhibition causes a dose-dependent accumulation of cells in the G0/G1 phase of the cell cycle. This G0/G1 arrest becomes significant at Ribociclib concentrations of 100 nM (p=0.007) and 250 nM (p=0.01), respectively. Treatment with Ribociclib obviously inhibits substrate adherent growth relative to the control in 12 of the 17 neuroblastoma cell lines examined (mean IC50=306±68 nM, considering sensitive lines only, where sensitivity is defined as an IC50 of less than 1 μM. Treating a panel of 17 neuroblastoma cell lines with Ribociclib across a four-log dose range (10 to 10,000 nM) [2]. |
| In vivo | Tumor growth is significantly delayed during 21 days of Ribociclib (LEE011; 200 mg/kg) treatment in mice with BE2C or 1643 xenografts (both, p<0.0001), although growth resumed post-treatment. CB17 immunodeficient mice with BE2C, NB-1643 (MYCN amplified, sensitive in vitro), or EBC1 (non-amplified, resistant in vitro) xenografts received daily treatment with Ribociclib or vehicle control, with no observed weight loss or toxicity signs in any models [2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 9 mg/mL (16.29 mM), Sonication is recommended.
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| Keywords | CDK | Ribociclib succinate | LEE 011 | Ribociclib | inhibit | LEE011 | LEE-011 Succinate | LEE-011 | Ribociclib Succinate | LEE 011 Succinate | Inhibitor | LEE011 Succinate | Cyclin dependent kinase |
| Inhibitors Related | Ribociclib | Ro-3306 | Rafoxanide | AT7519 | CASIN | Palbociclib | GW 441756 | Abemaciclib | Dinaciclib | Abemaciclib methanesulfonate |
| Related Compound Libraries | Bioactive Compound Library | EMA Approved Drug Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
