| 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/Shipping at ambient temperature. |
| Solubility Information | DMSO : 9 mg/mL (16.29 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween-80+45% Saline : 0.5 mg/mL (0.9 mM), Sonication is recommended.
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| Keywords | Ribociclib succinate | Ribociclib | LEE-011 Succinate | LEE011 Succinate | LEE-011 | LEE011 | LEE 011 Succinate | LEE 011 | Inhibitor | inhibit | Cyclin dependent kinase | CDK6 | CDK4 | CDK |
| Inhibitors Related | Ribociclib | (E)-β-Farnesene | Amantadine | 2-Chloropyrazine | Kojic acid | Abemaciclib | 2,4,6-Trihydroxybenzoic acid | Palbociclib | Abemaciclib methanesulfonate | Sodium Oxamate | Seliciclib | Dinaciclib |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Kinase Inhibitor Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
