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O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) 是 Midostaurin 的活性代谢物,通过细胞色素 P450 肝酶代谢产生,可以作为 Midostaurin 在体内代谢的指标之一。Midostaurin 是一种多靶点蛋白激酶 (kinase) 抑制剂,IC50 范围为 22-500 nM。
O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo[1]. Midostaurin is a multi-targeted protein kinase inhibitor with IC50 ranging from 22-500 nM.
[1]. Levis M, et al. Plasma inhibitory activity (PIA): a pharmacodynamic assay reveals insights into the basis for cytotoxic response to FLT3 inhibitors.Blood. 2006 Nov 15;108(10):3477-83.
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