BS 181 dihydrochloride
Biological Activity
Selective cdk7 inhibitor (IC50 = 21 nM). Displays >40-fold selectivity for cdk7 over others cdks. Promotes cell cycle arrest and apoptosis in a range of cancer cells in vitro and inhibits MCF-7 tumor xenograft growth in mice.
Compound Libraries
BS 181 dihydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 453.45 |
| Formula | C22H32N6.2HCl |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| PubChem ID | 91826108 |
| InChI Key | XYXAMTBYYTXHSO-UHFFFAOYSA-N |
| Smiles | CC(C)C1=C2N=C(NCCCCCCN)C=C(NCC3=CC=CC=C3)N2N=C1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.34 | 100 | |
| ethanol | 22.67 | 50 | |
| water | 45.34 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 453.45. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.21 mL | 11.03 mL | 22.05 mL |
| 5 mM | 0.44 mL | 2.21 mL | 4.41 mL |
| 10 mM | 0.22 mL | 1.1 mL | 2.21 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Ali et al (2009) The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity. Cancer Res. 69 6208 PMID: 19638587
If you know of a relevant reference for BS 181 dihydrochloride, please let us know.
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Citations for BS 181 dihydrochloride
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Literature in this Area
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
