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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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| Senexin B
Senexin B is a potent, orally active CDK8/19 inhibitor with Kd values of 140 nM and 80 nM for CDK8 and CDK19, respectively. |
| Q901
Q901 is a CDK7 inhibitor for tumor-related studies. |
| NUV-422
NUV-422 is a CDK2/4/6 inhibitor that can be used in studies related to malignant gliomas. |
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