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7-hydroxystaurosporine
- Development stage
- Phase 2
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
7-hydroxystaurosporine is a synthetic derivative of staurosporine with potent antineoplastic (anticancer) activity. It acts as a broad-spectrum protein kinase inhibitor, targeting multiple kinases including serine/threonine kinase AKT, calcium-dependent protein kinase C (PKC), cyclin-dependent kinases (CDKs), checkpoint kinase Chk1, and others. By inhibiting these kinases, it disrupts cell cycle progression—arresting tumor cells at the G1/S phase—and impairs DNA repair mechanisms by inhibiting the G2 checkpoint via Chk1 inhibition, ultimately leading to apoptosis. The drug has been investigated in clinical trials for various advanced solid tumors and hematologic malignancies[1][2][5][10].
- Other names
- 7-hydroxystaurosporine112953-11-4
02
Targets
CHEK2 (Checkpoint kinase 2)AKT (RAC-alpha serine/threonine-protein kinase)CDK1 (Cyclin-dependent kinase 1)PDK (Pyruvate dehydrogenase kinase isoform 1)PKC (Protein kinase C family)CDK2 (Cyclin-dependent kinase 2)CDK5 (Cyclin-dependent kinase 5)LCK (Proto-oncogene tyrosine-protein kinase Lck)CHEK1 (Checkpoint kinase 1)GSK3 (Glycogen synthase kinase 3 beta)MAPK14 (p38 mitogen-activated protein kinase alpha)PKA (Cyclic amp-dependent protein kinase)
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