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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.
In vivo, BS-181 (5 mg/kg, 10 mg/kg, i.p.) inhibits the growth of MCF-7 tumors in nude mice. Intravenous (i.v) and i.p administration of 10 mg/kg BS-181 shows rapid clearance. BS-181 (10 mg/kg/d or 20 mg/kg/d, i.p.) significantly inhibits the growth of tumor in a dose-dependent manner compared to the control group.
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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 |
| Cell Experiment | |
|---|---|
| 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 Experiment | |
|---|---|
| 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 |
| Molecular Weight | 416.99 |
| Formula | C22H32N6.HCl |
| CAS Number | 1397219-81-6 |
| Solubility (25°C) | Water 85 mg/mL DMSO 45 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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