Midostaurin

CAT: 0804-HY-10230-01Size: 1 mgDry Ice: NoHazardous: No
CAT#:0804-HY-10230-01Size:1 mg
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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].
CAS Number
[120685-11-2]
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

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