Midostaurin_product_DataBase

Bioactivity	Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM[1][2]. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects[3].
Invitro	Midostaurin (PKC412) shows a broad antiproliferative activity against various tumor and normal cell lines in vitro, and is able to reverse the Pgp-mediated multidrug resistance of tumor cells in vitro. Exposure of cells to Midostaurin (PKC412) results in a dose-dependent increase in the G2/M phase of the cell cycle concomitant with increased polyploidy, apoptosis and enhanced sensitivity to ionizing radiation[1]. Midostaurin (PKC412) induces substantial inhibition of KIT-, Lyn-, and STAT5 activity, but does not suppress Btk in HMC-1 cells and primary neoplastic mast cells[3]. Midostaurin (PKC412) inhibits EN fusion tyrosine kinase in hematopoietic Ba/F3 cells. Midostaurin (PKC412) significantly inhibits EN phosphorylation in M0-91 and IMS-M2 cells in a dose-dependent manner[4].
Name	Midostaurin
CAS	120685-11-2
Formula	C35H30N4O4
Molar Mass	570.64
Transport	Room temperature in continental US; may vary elsewhere.
Storage	-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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