BS-181 hydrochloride is a selective cyclin-dependent kinase inhibitor with an IC50 of 21 nM for the inhibition of CDK-activating kinase. Testing of other CDKs as well as another 69 kinases showed that BS-181 hydrochloride only inhibited CDK2 at concentrations lower than 1 μM, with CDK2 being inhibited 35-fold less potently (IC50 880 nM) than CDK7. In MCF-7 cells, BS-181 hydrochloride inhibited the phosphorylation of CDK7 substrates, promoted cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines, and showed antitumor effects in vivo.
|Cell lines||MCF-7 cells|
|Preparation method||Exposing MCF-7 cells to BS-181 for 24 hours. For the determination of cell cycle and apoptosis, staining cells with propidium iodide or labeled with Annexin V-FITC, then acquiring labeled cells within 1 hour, by using the RXP cytomics software on a Beckman Coulter Elite ESP, and using Flow Jo v7.2.5 to analyze the data . For the assessment of CDKs, lysing and analyzing cells by western blotting.|
|Concentrations||Dissolved in DMSO, final concentration ~50 μM|
|Incubation time||24 hours|
|Animal models||MCF-7 cells are established in female nu/nu-BALB/c athymic nude mice|
|Formulation||Prepared in the vehicle of 10% DMSO / 50 mM HCl / 5% Tween 20 / 85% saline.|
|Dosages||10 or 20 mg/kg|
|Administration||Twice daily by i.p. injection|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 80 mg/mL|
|Source||Drug Des Devel Ther (2016). Figure 1. BS-181|
|Method||Cell migration and invasion assay|
|Cell Lines||BGC 823 cells|
|Concentrations||1, 10, 20 μM|
|Incubation Time||24 h|
|Results||As expected, BS-181 significantly inhibited cell migration and invasion ability in a dose-dependent manner|
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