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Ribociclib (LEE011) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is 1000 times less active against cyclin B/CDK1 complex.
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Source | Bio Pharma (2018). Figure 5. LEE011 |
| Method | qRT-PCR | |
| Cell Lines | MDCKII-ABCB1, MDCKII-ABCG2, or MDCKII-parent cells | |
| Concentrations | 12 and 20 μM | |
| Incubation Time | 72 h | |
| Results | The ABCB1 and ABCG2 expression rate was assessed using the ΔΔCt method, and we observed no significant change in the transporter-encoding gene studied, as demonstrated in Figure 5D. |
| Cell Experiment | |
|---|---|
| Cell lines | MYCN amplified neuroblastoma cell lines |
| Preparation method | Pharmacologic growth inhibition LEE011 was provided by Novartis pharmaceuticals. A panel of neuroblastoma cell lines, selected based upon prior demonstration of substrate adherent growth, was plated in triplicate on the Xcelligence Real-Time Cell Electronic Sensing system (ACEA Biosciences) and treated 24 hours later with a four-log dose range of inhibitor or with a DMSO control. Cell indexes were monitored continuously for ~100 hours, and IC50 values were determined as follows: Growth curves were generated by plotting the cell index as a function of time and were 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 post-treatment was then calculated using a baseline area of 1 (the cell index at the time of treatment). Areas were normalized to the DMSO control, and the resulting data were analyzed using a non-linear log inhibitor vs. normalized response function (Graphpad). All experiments were repeated at least once. |
| Concentrations | 0~10µM |
| Incubation time | 96h |
| Animal Experiment | |
|---|---|
| Animal models | BE2C, NB-1643, or EBC1 cell line-derived xenografts of CB17 SCID−/− mice |
| Formulation | 0.5 % methylcellulose |
| Dosages | 200 mg/kg |
| Administration | oral |
| Molecular Weight | 434.54 |
| Formula | C23H30N8O |
| CAS Number | 1211441-98-3 |
| Solubility (25°C) | DMSO 10 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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PD-0332991 HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. |
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