CDK4/6/1 Inhibitor
Modify Date: 2024-01-13 18:38:51
CDK4/6/1 Inhibitor structure
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Common Name | CDK4/6/1 Inhibitor | ||
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| CAS Number | 2099128-41-1 | Molecular Weight | 488.57 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C28H30F2N6 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of CDK4/6/1 InhibitorCDK4/6/1 Inhibitor is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively. |
| Name | CDK4/6/1 Inhibitor |
|---|
| Description | CDK4/6/1 Inhibitor is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively. |
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| Related Catalog | |
| Target |
IC50: 3 nM (CDK4), 1 nM (CDK6)[1] |
| In Vitro | CDK4/6/1 Inhibitor is a potent anti-proliferative agent that arrests U87MG cell line exclusively in G1 (IC50=15.3 ± 2.9 nM in the anti-proliferation assay). U87MG cells exposed to varying concentrations of CDK4/6/1 Inhibitor for 24 hours show a dose-related increase in G1 arrest, and a significant increase in the percentage of cells in G1 is found in as little as 13.72 nM of CDK4/6/1 Inhibitor[1]. |
| In Vivo | CDK4/6/1 Inhibitor has tumor growth inhibition values ranging from 62% to 99% for doses ranging from 3.125 to 50 mg/kg in an orthotopic xenograft mouse model of glioblastoma multiforme, and no significant body weight loss is observed. The increase in life span based on the median survival time of vehicle-treated animals in mice administered a dose of 50 mg/kg is significant at 162%[1]. |
| Cell Assay | The U87MG glioblastoma cells are treated with CDK4/6/1 and incubated for 72 h at 37°C. Then the medium is removed, 4% paraformaldehyde (50 µL/well) is added to the wells, and the cells are fixed for 30 min at RT. Cells are washed twice with phosphate-buffered saline (PBS) solution, and permeabilized in 0.2% Triton-X100 for 5 min. Cells are ished twice with PBS, after which 50 µL DAPI (1 µg/mL) is added to the wells, followed by incubation of the cells in the dark for 20 min. After ishing three times with PBS, PBS (100 µL/well) is added to the wells. The plates are scanned using IN Cell Analyzer 2200[1]. |
| Animal Admin | Mice[1] In the U87MG-Luc orthotopic xenograft mouse model, mice are treated with 3.125, 6.25, 12.5, 25, 50 mg/kg QD CDK4/6/1 Inhibitor for 28 days |
| References |
| Molecular Formula | C28H30F2N6 |
|---|---|
| Molecular Weight | 488.57 |