MedKoo product information:

  BAY1000394

Description of BAY1000394: BAY10-00394 is an orally bioavailable cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. pan-CDK inhibitor BAY1000394 selectively binds to and inhibits the activity of CDK1/Cyclin B, CDK2/Cyclin E, CDK4/Cyclin D1, and CDK9/Cyclin T1, serine/threonine kinases that play key roles in the regulation of the cell cycle progression and cellular proliferation. Inhibition of these kinases leads to cell cycle arrest during the G1/S transition, thereby leading to an induction of apoptosis, and inhibition of tumor cell proliferation. CDKs are often dysregulated in cancerous cells. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:    Bayer.

BAY1000394 Inhibited proliferation with a mean IC50 of 16 nM (8–37 nM). Activity independent of functional p53 or RB. Reduced phosphorylation of RB in vitro and in xenografts, indicating intracellular inhibition of CDK2 and CDK4. Reduced RB phosphorylation in paclitaxel- and cisplatin-refractory xenografts [source: Nature Reviews Cancer 11, 558-572 (August 2011)]