Samuraciclib hydrochloride is a potent, selective, ATP-competitive, and orally active CDK7 inhibitor with an IC50 of 41 nM. It exhibits selectivity over CDK1, CDK2, CDK5, and CDK9. This compound inhibits the growth of breast cancer cell lines and demonstrates anti-tumor effects, promoting cell apoptosis and inducing cell cycle arrest.
- Potent and selective CDK7 inhibitor (IC50 41 nM)
- Shows selectivity over CDK1, CDK2, CDK5, and CDK9
- Inhibits growth of breast cancer cell lines (GI50 0.2-0.3 μM)
- Promotes cell apoptosis and induces cell cycle arrest
- Inhibits PolII CTD phosphorylation
- Demonstrates anti-tumor effects in animal models
- Leads to complete growth arrest of ER-positive tumor xenografts in combination therapy