| Description |
CDK4/6/1 Inhibitor is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively.
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| Related Catalog |
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| Target |
IC50: 3 nM (CDK4), 1 nM (CDK6)[1]
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| 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].
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| 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].
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| 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].
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| 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
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| References |
[1]. Yin L, et al. A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy. Eur J Med Chem. 2018 Jan 20;144:1-28.
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