1. Epigenetics
    TGF-beta/Smad
    Protein Tyrosine Kinase/RTK
    Immunology/Inflammation
    Apoptosis
  2. PKC
    VEGFR
    c-Kit
    NO Synthase
    Apoptosis
  3. Midostaurin

Midostaurin (Synonyms: PKC412; CGP 41251)

Cat. No.: HY-10230 Purity: 99.89%
Handling Instructions

Midostaurin (PKC412; CGP 41251) est un inhibiteur de protéine kinase multi-ciblé qui inhibe PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ et VEGFR1/2 avec des IC50s allant de 22 -500 nM.

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. Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects.

For research use only. We do not sell to patients.

Midostaurin Chemical Structure

Midostaurin Chemical Structure

CAS No. : 120685-11-2

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 126 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 126 In-stock
Estimated Time of Arrival: December 31
Solid
1 mg USD 60 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 770 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Midostaurin:

Top Publications Citing Use of Products

    Midostaurin purchased from MCE. Usage Cited in: Haematologica. 2018 Nov;103(11):1862-1872.

    Induction of tumor suppressor protein p53 in MV4-11 (A) and MOLM-13 cells (B) treated for 24 hours with the indicated amounts of NVP-HDM201 and midostaurin. Relative quantitation of CDKN1A mRNA (C) and MCL-1 mRNA (D) in AML cells treated for 24 hours with PKC412 and NVP-HDM201 alone or in combination.

    Midostaurin purchased from MCE. Usage Cited in: J Cell Mol Med. 2020 Feb;24(3):2145-2156.

    Effects of Midostaurin in vivo against mice harbouring Ba/F3.FLT3(wt).CBL.Y371H-luc+ cells. Supine and Prone (High Scale), Days 12-19. Representative Images (n = 5).
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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].

    IC50 & Target[2]

    cPKC-α

    22 nM (IC50)

    cPKC-γ

    24 nM (IC50)

    cPKC-β1

    30 nM (IC50)

    cPKC-β2

    31 nM (IC50)

    nPKC-δ

    33 nM (IC50)

    nPKC-η

    160 nM (IC50)

    nPKC-ε

    1250 nM (IC50)

    aPKC-ζ

    465000 nM (IC50)

    PPK

    38 nM (IC50)

    KDR

    86 nM (IC50)

    c-Syk

    95 nM (IC50)

    cdk1/cycB

    570 nM (IC50)

    Protein kinase A

    570 nM (IC50)

    c-Fgr

    790 nM (IC50)

    c-Src

    800 nM (IC50)

    Flt-1

    912 nM (IC50)

    EGF-R

    1100 nM (IC50)

    Myosin-light chain kinase

    1900 nM (IC50)

    Flk-1

    3900 nM (IC50)

    c-Lyn

    4300 nM (IC50)

    P70S6 kinase

    5000 nM (IC50)

    CSK

    8000 nM (IC50)

    In Vitro

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    Midostaurin (PKC412) strongly inhibits retinal neovascularization as well as laser-induced choroidal neovascularization in murine models[1]. Midostaurin (PKC412) (25 mg/kg, i.p.) protects mouse livers of the K18 Arg90Cys-overexpressing transgenic mice from Fas-induced apoptosis[5].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    570.64

    Formula

    C35H30N4O4

    CAS No.
    SMILES

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

    Shipping

    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)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (87.62 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7524 mL 8.7621 mL 17.5242 mL
    5 mM 0.3505 mL 1.7524 mL 3.5048 mL
    10 mM 0.1752 mL 0.8762 mL 1.7524 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.38 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.38 mM); Clear solution

    *All of the co-solvents are available by MCE.
    References
    Cell Assay
    [3]

    Proliferation is determined by trypan blue dye exclusion test. Cells in suspension are seeded in six-well plates at a density of 1×105 cells/mL in the presence of different concentrations of PKC412 for 3 days. In control wells, DMSO instead of Midostaurin (PKC412) is added. After the treatment, 10 μL of the cell suspension is mixed with 10 μL of 0.4% trypan blue, and alive cells are counted manually using a hemacytometer. Results are calculated as the percentage of the values measured when cells are grown in the absence of the reagent. All experiments are performed in triplicate[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [4]

    K8-deficient, K18-deficient, and human K18 R90C-overexpressing mice with age of 6-8 weeks are used in the assay. Age and sex matched mice are treated with Midostaurin (25 mg/kg), daily for 4 d or with an equal volume of DMSO as vehicle (both administered intraperitoneally). On day 5 post-treatment, apoptosis is induced by intraperitoneal injection of Fas ligand (Fas-L) (0.15 μg/g body weight). Mice are fasted overnight before Fas Ab injection, and 18 mice are used per DMSO or Midostaurin (PKC412) group for the Fas-treated mice while 6 mice are used per DMSO or Midostaurin (PKC412) group for the control non-Fas-treated mice. Mice are sacrificed by CO2 inhalation 6 h after Fas Ab injection. Blood is collected by intracardiac puncture, and livers are harvested for hematoxylin and eosin (HE) staining (after fixation in 10% formalin) or frozen in optimum cutting temperature compound for immunofluorescence staining[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.89%

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