| Name | Ribociclib |
| Description | Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor (IC50:10/39 nM). |
| Cell Research | A panel of neuroblastoma cell lines, selected based upon prior demonstration of substrate adherent growth, is plated in triplicate on the Xcelligence Real-Time Cell Electronic Sensing system and treated 24 hours later with a four-log dose range of inhibitor or with a dimethyl sulfoxide (DMSO) control. Cell indexes are monitored continuously for ~100 hours, and IC50 values are determined as follows: growth curves are generated by plotting the cell index as a function of time and are normalized to the cell index at the time of treatment for a baseline cell index of 1. The area under the normalized growth curve from the time of treatment to 96 hours posttreatment is then calculated using a baseline area of 1 (the cell index at the time of treatment). Areas are normalized to the DMSO control, and the resulting data are analyzed using a nonlinear log inhibitor versus normalized response function. All experiments are repeated at least once. (Only for Reference) |
| Kinase Assay | Enzyme assays are performed using a homogeneous time-resolved fluorescence assay with recombinant epitope tagged kinase domains (JAK1, 837-1142; JAK2, 828-1132; JAK3, 718-1124; Tyk2, 873-1187) or full-length enzyme (cMET and Chk2) and peptide substrate. Each enzyme reaction is performed with or without test compound (11-point dilution), JAK, cMET, or Chk2 enzyme, 500 nM (100 nM for Chk2) peptide, ATP (at the Km specific for each kinase or 1 mM), and 2.0% DMSO in assay buffer. The calculated IC50 value is the compound concentration required for inhibition of 50% of the fluorescent signal. Additional kinase assays are performed at Cerep using standard conditions at 200 nM. Enzymes tested included: Abl, Akt1, AurA, AurB, CDC2, CDK2, CDK4, CHK2, c-kit, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKKα, IKKβ, JNK1, Lck, MEK1, p38α, p70S6K, PKA, PKCα, Src, and ZAP70[1]. |
| In vitro | LEE011 (200 mg/kg/day, p.o.) significantly delayed the growth of BE2C or 1643 cells in mice without causing weight loss or other toxic symptoms. |
| In vivo | LEE011 inhibits the growth of neuroblastoma cells, a process regulated by G1 cell cycle arrest and cellular senescence. It demonstrates significant growth suppression in 12 out of 17 neuroblastoma types evaluated, with an average IC50 of 307 nM. |
| Storage | Store under nitrogen | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 9 mg/mL (20.71 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (11.51 mM), Suspension.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | VEGFR6 | VEGFR4 | Ribociclib | LEE-011 | LEE 011 | Inhibitor | inhibit | Cyclin dependent kinase | CDK4 | CDK |
| Inhibitors Related | 2-Chloropyrazine | Kojic acid | Sorafenib | Abemaciclib | glycine | Nintedanib esylate | Regorafenib | Ethyl cinnamate | Palbociclib | Sodium Oxamate | Lenvatinib | Pazopanib |
| Related Compound Libraries | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
