Bioactivity | (rac)-ZK-304709 is an isomer of ZK-304709. It is a first-in-class oral multi-target tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (Cdks), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. It directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. In an orthotopic BON tumor model, (rac)-ZK-304709 reduced primary tumor growth by 80% and reduced tumor microvascular density. These results suggest that (rac)-ZK-304709 can effectively control tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may be a potential agent for the treatment of NET. |
CAS | 1010440-84-2 |
Formula | C22H29ClN6O2 |
Molar Mass | 444.96 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. The oral multitarget tumour growth inhibitor, ZK 304709, inhibits growth of pancreatic neuroendocrine tumours in an orthotopic mouse model |