7-oxo Staurosporine is an antibiotic originally isolated from S. platensis with diverse biological activites. It inhibits PKC, PKA, phosphorylase kinase, EGFR, and c-Src in vitro (ICs = 9, 26, 5, 200, and 800 nM, respectively). 7-oxo Staurosporine induces cell cycle arrest in the G/M phase in human leukemia K562 cells with a minimal effective dose (MED) of 30 ng/ml. It is cytotoxic to P388 mouse leukemia cells that are resistant and susceptible to doxorubicin . 7-oxo Staurosporine inhibits growth of the mycelial, but not yeast form of C. albicans, C. krusei, C. tropicalis, and C. lusitaniae (MICs = 3.1-25 μg/ml). It increases sphingomyelin synthesis in CHO-K1 cells when used at a concentration of 50 nM.
7-Oxostaurosporine is a potent protein kinase C (PKC) inhibitor that effectively inhibits tumor growth by inducing apoptosis and inhibiting the nuclear factor (NF)-κB/p-p65 pathway.
体外研究
7-Oxostaurosporine (50 nM, 24 h) can lead to an increase in plasma membrane sphingomyelin in CHO cells but does not alter ceramide content.
体内研究
7-Oxostaurosporine (6 mg/kg, once daily, intravenous) significantly reduces tumour growth with a tumour growth inhibition (TGI) of 56.1% and no significant effect on body weigh.
分子式
C28H24N4O4
分子量
480.5
CAS号
125035-83-8
中文名称
7-氧代星形孢菌素
运输条件
Room temperature in continental US; may vary elsewhere.