3-Hydroxy Midostaurin  (Synonyms: CGP52421)

3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC₅₀s 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^[1].

IC50: 132 nM (FLT3 in culture medium) and 9.8 μM (FLT3 in plasma)^[1]

CGP52421 (200, 400, 600, 800, 1000 nM) is more cytotoxic than PKC412 over the dose range 100 to 500 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

586.64

C₃₅H₃₀N₄O₅

179237-49-1

Solid

Light yellow to yellow

OC1NC(C2=C1C(C3=C4C=CC=C3)=C5N4[C@]6(O[C@@H](N7C5=C2C8=C7C=CC=C8)C[C@H]([C@H]6OC)N(C(C9=CC=CC=C9)=O)C)C)=O

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]