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Overview
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Background
Midostaurin is an inhibitor of PKC with IC50 values of 22nM, 30nM, 31nM, 24nM, 330nM, 160nM and 1.25μM for PKC-α, PKC-β1, PKC-β2, PKC-γ, PKC-δ, PKC-η and PKC-ε, respectively [1].Midostaurin is a PKC inhibitor with potent activity against most PKC subtypes. It also has inhibitory activity against KDR and its mouse homologue Flk-1. Other protein kinases involved in angiogenesis, cell cycle and cell growth are not sensitive to midostaurin. Midostaurin shows reversible inhibition of intracellular PKC activity with IC50 value of 0.5μM. Besides PKC, midostaurin inhibits the autophosphorylation of the receptors for PDGF, VEGF and stem cell factor with IC50 values of 80nM, 1μM and 30nM, respectively. Midostaurin also inhibits the FGF-induced c-fos transcription and MAPK activation. Moreover, midostaurin suppresses cell growth of different cell lines through inducing cell cycle arrest in G2/M and inducing apoptosis [1]. Furthermore, midostaurin exerts antitumor activity via inhibiting tumor angiogenesis and proliferation due to its effects on VEGFR and PKC, respectively. Administration of midostaurin prolongs the life span of mice bearing B16 melanoma at dose of 75mg/kg 3 times daily for 9 days [1].
[1] Fabbro D, Buchdunger E, Wood J, et al. Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent. Pharmacology & therapeutics, 1999, 82(2): 293-301.
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