Midostaurin

• Description:

  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 Name Alternative:

  PKC412; CGP 41251

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H315, H319, H335

• Target:

  Apoptosis; c-Kit; NO Synthase; PKC; VEGFR

• Type:

  Reference compound

• Related Pathways:

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

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/PKC412.html

• Purity:

  99.91

• Solubility:

  DMSO : 50 mg/mL (ultrasonic)

• Smiles:

  O=C (C1=CC=CC=C1) N (C) [C@H]2[C@@H] (OC) [C@@]3 (C) N (C4=C5C=CC=C4) C6=C5C7=C (C (NC7) =O) C8=C6N (C9=CC=CC=C98) [C@@] (O3) ([H]) C2

• Molecular Formula:

  C35H30N4O4

• Molecular Weight:

  570.64

• Precautions:

  H302, H315, H319, H335

• 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]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.|[5]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.|[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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C (Powder, sealed storage, away from moisture)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Isoform:

  ENOS; PKCα; PKCβ; PKCγ; PKCδ; PKCε; PKCζ; PKCη

• CAS Number:

  120685-11-2