3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC 50 s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412.
性状
Solid
IC50 & Target[1][2]
IC50: 132 nM (FLT3 in culture medium) and 9.8 μM (FLT3 in plasma)
体外研究(In Vitro)
CGP52421 (200, 400, 600, 800, 1000 nM) is more cytotoxic than PKC412 over the dose range 100 to 500 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.