Midostaurin (Synonyms: PKC412; CGP 41251)

Name: Midostaurin
Brand: MedChemExpress
SKU: HY-10230
Rating: 5.0 (28 reviews)

Cat. No.: HY-10230 Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 120685-11-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 126	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	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

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 28 publication(s) in Google Scholar

Other Forms of Midostaurin:

Midostaurin-d₅ Get quote
Midostaurin (Standard) Get quote

26 Publications Citing Use of MCE Midostaurin

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

: Midostaurin purchased from MedChemExpress. Usage Cited in: Haematologica. 2018 Nov;103(11):1862-1872. [Abstract]; 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.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PKC Isoform Specific Products:

View All Isoforms

PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

View All VEGFR Isoform Specific Products:

View All Isoforms

VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

View All NO Synthase Isoform Specific Products:

View All Isoforms

nNOS iNOS eNOS

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)

eNOS

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)

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	180 nM Compound: PKC-412	Toxicity against human A375 cells after 72 hrs by cell titer-blue assay Toxicity against human A375 cells after 72 hrs by cell titer-blue assay	[PMID: 19654408]
BaF3	GI₅₀	< 10 nM Compound: 1c	Growth inhibition of mouse BAF3 cells harboring FLT3 measured after 72 hrs by CCK8 assay Growth inhibition of mouse BAF3 cells harboring FLT3 measured after 72 hrs by CCK8 assay	[PMID: 35923716]
BaF3	IC₅₀	< 10 nM Compound: 1c	Induction of cell cycle arrest at G1 phase in mouse BaF3 cells harboring FLT3 ITD assessed as accumulation of cells at G1 phase measured after 72 hrs by flow cytometry method Induction of cell cycle arrest at G1 phase in mouse BaF3 cells harboring FLT3 ITD assessed as accumulation of cells at G1 phase measured after 72 hrs by flow cytometry method	[PMID: 35923716]
BaF3	IC₅₀	< 10 nM Compound: 1c	Induction of apoptosis in mouse BaF3 cells harboring FLT3 ITD mutation measured after 72 hrs by Annexin-V-Fluos Staining Kit analysis Induction of apoptosis in mouse BaF3 cells harboring FLT3 ITD mutation measured after 72 hrs by Annexin-V-Fluos Staining Kit analysis	[PMID: 35923716]
BaF3	GI₅₀	< 100 nM Compound: 1c	Growth inhibition of mouse BAF3 cells measured after 72 hrs by CCK8 assay Growth inhibition of mouse BAF3 cells measured after 72 hrs by CCK8 assay	[PMID: 35923716]
BaF3	GI₅₀	16 nM Compound: 4; PKC412	Inhibition of FLT3 D835Y mutant in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Inhibition of FLT3 D835Y mutant in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 31721578]
BaF3	IC₅₀	4.14 nM Compound: Midostaurin	Antiproliferative activity against mouse BaF3 FLT3-ITD cells assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against mouse BaF3 FLT3-ITD cells assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 32659083]
BaF3	GI₅₀	43 nM Compound: 4; PKC412	Inhibition of FLT3 ITD/D835Y double mutant in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Inhibition of FLT3 ITD/D835Y double mutant in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 31721578]
BaF3	GI₅₀	47 nM Compound: 4; PKC412	Inhibition of FLT3 ITD/F691L double mutant in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Inhibition of FLT3 ITD/F691L double mutant in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 31721578]
BaF3	GI₅₀	540 nM Compound: 4; PKC412	Cytotoxicity against mouse BAF3 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Cytotoxicity against mouse BAF3 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 31721578]
EOL1	IC₅₀	0.0038 μM Compound: PKC412	Cytotoxicity against human EOL-1 cells after 72 hrs by MTS assay Cytotoxicity against human EOL-1 cells after 72 hrs by MTS assay	[PMID: 29350920]
GISTT1	GI₅₀	235 nM Compound: 4; PKC412	Antiproliferative activity against human GISTT1 cells harboring heterozygous deletion mutation at C-kit exon 11 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Antiproliferative activity against human GISTT1 cells harboring heterozygous deletion mutation at C-kit exon 11 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 31721578]
HL-60	IC₅₀	> 10 μM Compound: PKC-412	Antiproliferative activity against human HL60 cells measured after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human HL60 cells measured after 72 hrs by Celltiter-Glo assay	[PMID: 31361136]
HL-60	IC₅₀	0.5 μM Compound: Midostaurin	Antiproliferative activity against human HL-60 cells expressing wild type FLT3 assessed as reduction in cell viability measured after 72 hrs by MTS assay Antiproliferative activity against human HL-60 cells expressing wild type FLT3 assessed as reduction in cell viability measured after 72 hrs by MTS assay	[PMID: 35148084]
HT-22	IC₅₀	1 μM Compound: 48	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 36876904]
K562	IC₅₀	> 10 μM Compound: PKC-412	Antiproliferative activity against human K562 cells measured after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human K562 cells measured after 72 hrs by Celltiter-Glo assay	[PMID: 31361136]
K562	GI₅₀	> 20 μM Compound: 1, PKC412	Inhibition of wild type BCR/ABL in FLT3 deficient human K562 cells assessed as cell growth inhibition after 72 hrs by MTS assay Inhibition of wild type BCR/ABL in FLT3 deficient human K562 cells assessed as cell growth inhibition after 72 hrs by MTS assay	[PMID: 26081023]
K562	GI₅₀	> 20000 nM Compound: 4; PKC412	Antiproliferative activity against human K562 expressing wild type BCR/ABL assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Antiproliferative activity against human K562 expressing wild type BCR/ABL assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 31721578]
Kasumi 1	GI₅₀	284 nM Compound: 4; PKC412	Antiproliferative activity against human Kasumi-1 harboring c-kit N822K mutant assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Antiproliferative activity against human Kasumi-1 harboring c-kit N822K mutant assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 31721578]
MOLM-13	IC₅₀	0.0047 μM Compound: PKC412	Cytotoxicity against human MOLM13 cells after 72 hrs by MTS assay Cytotoxicity against human MOLM13 cells after 72 hrs by MTS assay	[PMID: 29350920]
MOLM-13	GI₅₀	0.055 μM Compound: 1, PKC412	Inhibition of FLT3 ITD heterozygous mutant in human MOLM-13 cells assessed as cell growth inhibition after 72 hrs by MTS assay Inhibition of FLT3 ITD heterozygous mutant in human MOLM-13 cells assessed as cell growth inhibition after 72 hrs by MTS assay	[PMID: 26081023]
MOLM-13	GI₅₀	55 nM Compound: 4; PKC412	Antiproliferative activity against human MOLM13 harboring FLT3-ITD mutant assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Antiproliferative activity against human MOLM13 harboring FLT3-ITD mutant assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 31721578]
MV4-11	GI₅₀	0.038 μM Compound: 1, PKC412	Inhibition of FLT3 ITD homozygous mutant in human MV4-11 cells assessed as cell growth inhibition after 72 hrs by MTS assay Inhibition of FLT3 ITD homozygous mutant in human MV4-11 cells assessed as cell growth inhibition after 72 hrs by MTS assay	[PMID: 26081023]
MV4-11	IC₅₀	0.04 μM Compound: PKC-412	Antiproliferative activity against human MV4-11 cells measured after 72 hrs by Celltiter-Glo assay Antiproliferative activity against human MV4-11 cells measured after 72 hrs by Celltiter-Glo assay	[PMID: 31361136]
MV4-11	IC₅₀	12 nM Compound: PKC-412	Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay	[PMID: 19654408]
MV4-11	GI₅₀	38 nM Compound: 4; PKC412	Antiproliferative activity against human MV4-11 harboring FLT3-ITD mutant assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Antiproliferative activity against human MV4-11 harboring FLT3-ITD mutant assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 31721578]
OCI-AML2	GI₅₀	6244 μM Compound: PKC412	Antiproliferative activity against patient derived OCI-AML2 cells harboring wild type FLT3 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against patient derived OCI-AML2 cells harboring wild type FLT3 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 30565931]
PBMC	IC₅₀	> 10 μM Compound: PKC-412	Cytotoxicity against human PBMC cells measured after 72 hrs by Celltiter-Glo assay Cytotoxicity against human PBMC cells measured after 72 hrs by Celltiter-Glo assay	[PMID: 31361136]
RS4-11	IC₅₀	13 nM Compound: PKC-412	Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay	[PMID: 19654408]
RS4-11	IC₅₀	15 nM Compound: PKC-412	Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay	[PMID: 19654408]
RS4-11	GI₅₀	400 nM Compound: 4; PKC412	Antiproliferative activity against human RS4:11 expressing native FLT3 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Antiproliferative activity against human RS4:11 expressing native FLT3 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 31721578]
Sf9	IC₅₀	0.037 μM Compound: 1, PKC412	Inhibition of wild type GST-tagged FLT3 kinase domain (Y567 to S993) (unknown origin) expressed in baculovirus infected insect Sf9 cells using Her2 peptide as substrate after 4 hrs by Kinase-Glo assay Inhibition of wild type GST-tagged FLT3 kinase domain (Y567 to S993) (unknown origin) expressed in baculovirus infected insect Sf9 cells using Her2 peptide as substrate after 4 hrs by Kinase-Glo assay	[PMID: 26081023]
Sf9	IC₅₀	0.08 μM Compound: 1, PKC412	Inhibition of recombinant GST-tagged Aurora-A kinase domain (S123 to S401) (unknown origin) expressed in insect Sf9 cells using tetra(LRRASLG) peptide as substrate after 90 mins by Kinase-Glo assay Inhibition of recombinant GST-tagged Aurora-A kinase domain (S123 to S401) (unknown origin) expressed in insect Sf9 cells using tetra(LRRASLG) peptide as substrate after 90 mins by Kinase-Glo assay	[PMID: 26081023]
Sf9	IC₅₀	0.25 μM Compound: 1, PKC412	Inhibition of recombinant GST-tagged VEGFR2 kinase domain (V789 to V1356) (unknown origin) expressed in insect Sf9 cells using polyGlu4:Tyr peptide as substrate after 120 mins by Kinase-Glo assay Inhibition of recombinant GST-tagged VEGFR2 kinase domain (V789 to V1356) (unknown origin) expressed in insect Sf9 cells using polyGlu4:Tyr peptide as substrate after 120 mins by Kinase-Glo assay	[PMID: 26081023]
Sf9	IC₅₀	109 nM Compound: 4; PKC412	Inhibition of recombinant N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) (unknown origin) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr) 4:1 as substrate measured after 150 mins in presence of Inhibition of recombinant N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) (unknown origin) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr) 4:1 as substrate measured after 150 mins in presence of	[PMID: 31721578]
Sf9	IC₅₀	40 nM Compound: 4; PKC412	Inhibition of wild type recombinant GST-tagged FLT3 (Y567 to S993 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using Her2 peptide as substrate measured after 4 hrs in presence of ATP by Kinase-Glo Plus reagent-based lumine Inhibition of wild type recombinant GST-tagged FLT3 (Y567 to S993 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using Her2 peptide as substrate measured after 4 hrs in presence of ATP by Kinase-Glo Plus reagent-based lumine	[PMID: 31721578]
U-937	GI₅₀	1.4 μM Compound: 1, PKC412	Cytotoxicity against FLT3-deficient human U937 cells assessed as cell growth inhibition after 72 hrs by MTS assay Cytotoxicity against FLT3-deficient human U937 cells assessed as cell growth inhibition after 72 hrs by MTS assay	[PMID: 26081023]
U-937	GI₅₀	1400 nM Compound: 4; PKC412	Antiproliferative activity against human U937 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay Antiproliferative activity against human U937 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay	[PMID: 31721578]

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].

MedChemExpress (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].

MedChemExpress (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.

120685-11-2

Appearance

Solid

Color

White to yellow

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

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.91%

Select Batch:

Data Sheet (289 KB) SDS (393 KB)

COA (261 KB) HNMR (274 KB) RP-HPLC (244 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Fabbro D, et al. PKC412--a protein kinase inhibitor with a broad therapeutic potential. Anticancer Drug Des. 2000 Feb;15(1):17-28. [Content Brief]

[2]. 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. [Content Brief]

[3]. 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. [Content Brief]

[4]. 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. [Content Brief]

[5]. 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. [Content Brief]

[6]. 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. [Content Brief]

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	[1]. Fabbro D, et al. PKC412--a protein kinase inhibitor with a broad therapeutic potential. Anticancer Drug Des. 2000 Feb;15(1):17-28. [Content Brief] [2]. 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. [Content Brief] [3]. 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. [Content Brief] [4]. 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. [Content Brief] [5]. 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. [Content Brief] [6]. 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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7524 mL	8.7621 mL	17.5242 mL	43.8105 mL
	5 mM	0.3505 mL	1.7524 mL	3.5048 mL	8.7621 mL
	10 mM	0.1752 mL	0.8762 mL	1.7524 mL	4.3810 mL
	15 mM	0.1168 mL	0.5841 mL	1.1683 mL	2.9207 mL
	20 mM	0.0876 mL	0.4381 mL	0.8762 mL	2.1905 mL
	25 mM	0.0701 mL	0.3505 mL	0.7010 mL	1.7524 mL
	30 mM	0.0584 mL	0.2921 mL	0.5841 mL	1.4603 mL
	40 mM	0.0438 mL	0.2191 mL	0.4381 mL	1.0953 mL
	50 mM	0.0350 mL	0.1752 mL	0.3505 mL	0.8762 mL
	60 mM	0.0292 mL	0.1460 mL	0.2921 mL	0.7302 mL
	80 mM	0.0219 mL	0.1095 mL	0.2191 mL	0.5476 mL

Midostaurin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社
Product Name			Salutation
Applicant Name *			Email Address *
Phone Number *			Organization Name *
Department *			Requested quantity *
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Midostaurin (Synonyms: PKC412; CGP 41251)

Customer Review

Other Forms of Midostaurin:

26 Publications Citing Use of MCE Midostaurin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PKC Isoform Specific Products:

View All VEGFR Isoform Specific Products:

View All NO Synthase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Midostaurin Related Classifications

Keywords:

Your Recently Viewed Products:

Name
Email *

	Sorry, but the email address you supplied was invalid.

Midostaurin (Synonyms: PKC412; CGP 41251)

Customer Review

Other Forms of Midostaurin:

Midostaurin Related Antibodies

26 Publications Citing Use of MCE Midostaurin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PKC Isoform Specific Products:

View All VEGFR Isoform Specific Products:

View All NO Synthase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Midostaurin Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Midostaurin Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report