Midostaurin-13C6

Midostaurin-13C6 (PKC412-13C6) is the 13C-labeled Midostaurin (HY-10230) . 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].

Product Specifications

Product Name Alternative

PKC412-13C6; CGP 41251-13C6

UNSPSC

12352005

Target

Apoptosis; c-Kit; Isotope-Labeled Compounds; NO Synthase; PKC; VEGFR

Related Pathways

Apoptosis; Epigenetics; Immunology/Inflammation; Others; Protein Tyrosine Kinase/RTK; TGF-beta/Smad

Field of Research

Cancer

Smiles

O=C(N([C@@H]1C[C@H]2O[C@@](C)([C@@H]1OC)N3C4=C(C5=C3C6=C(C7=C(N26)C=CC=C7)C8=C5CNC8=O)C=CC=C4)C)[13C]9=[13CH][13CH]=[13CH][13CH]=[13CH]9

Molecular Formula

C29 13C6H30N4O4

Molecular Weight

576.59

References & Citations

[1]Fabbro D, et al. PKC412--a protein kinase inhibitor with a broad therapeutic potential. Anticancer Drug Des. 2000 Feb;15 (1) :17-28.|[2]Gleixner KV, et al. Synergistic growth-inhibitory effects of Midostaurin (PKC412) on neoplastic mast cells carrying KIT D816V. Haematologica. 2013 Sep;98 (9) :1450-7.|[3]Chi HT, et al. ETV6-NTRK3 as a therapeutic target of small molecule inhibitor PKC412. Biochem Biophys Res Commun. 2012 Dec 7;429 (1-2) :87-92.|[4]Fabbro D, et al. Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent. Pharmacol Ther. 1999 May-Jun;82 (2-3) :293-301.|[5]Kwan R, et al. PKC412 normalizes mutation-related keratin filament disruption and hepatic injury in mice by promoting keratin-myosin binding. Hepatology. 2015 Dec;62 (6) :1858-69.|[6]Huige Li, et al. Midostaurin upregulates eNOS gene expression and preserves eNOS function in the microcirculation of the mouse. Nitric Oxide. 2005 Jun;12 (4) :231-6.