3-Hydroxy Midostaurin

Names

[ Name ]:
3-Hydroxy Midostaurin

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3

[Target]

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

[In Vitro]

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

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₅H₃₀N₄O₅

[ Molecular Weight ]:
586.63600

[ Exact Mass ]:
586.22200

[ PSA ]:
97.96000

[ LogP ]:
5.72650

Related Compounds

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