BMS-863233

BMS-863233, also known as XL413, is an orally bioavailable small molecule inhibitor of cell division cycle 7-related protein kinase (CDC7). It acts as a potent and selective ATP competitive inhibitor of CDC7 kinase (IC50 = 3.4 nM), a serine-threonine kinase essential for the initiation of DNA replication by activating origins of replication. Inhibition of CDC7 by BMS-863233 leads to suppression of DNA replication and mitosis, induction of tumor cell apoptosis, and inhibition of proliferation in tumor cells that overexpress CDC7. The drug was developed for potential antineoplastic activity in various cancers including refractory hematologic cancer and advanced/metastatic solid tumors. Initial clinical development was sponsored by Bristol Myers Squibb in collaboration with Exelixis; however, early trials were terminated due to pharmacokinetic issues and lack of efficacy. More recently, BMS‑863233 has been investigated in combination with chemotherapy for its anticancer effects[1][2][3][4][5][7].

Other names

UNII-8QK62S7492UNII8QK62S7492UNII 8QK62S7492