Midostaurin (Synonyms: 米哚妥林; PKC412; CGP 41251)

目录号: HY-10230 纯度: 99.91%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Midostaurin (PKC412; CGP 41251) 是一种具有口服活性的可逆多靶点蛋白激酶抑制剂。Midostaurin 抑制 PKCα/β/γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ 和 VEGFR1/2，IC₅₀ 范围为 22-500 nM。Midostaurin 还上调内皮一氧化氮合酶 (eNOS) 基因表达。Midostaurin 显示出强大的抗癌作用。

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Midostaurin Chemical Structure

CAS No. : 120685-11-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2260	In-stock
1 mg	￥770	In-stock
5 mg	￥1800	In-stock
10 mg	￥2880	In-stock
25 mg	￥4523	In-stock
50 mg	现货	询价
100 mg		询价
200 mg		询价

or 大包装询价

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Customer Review

Other Forms of Midostaurin:

Midostaurin-d₅ In-stock
Midostaurin (Standard) 询价

MCE 顾客使用本产品发表的 26 篇科研文献

: Midostaurin purchased from MCE. 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 MCE. 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.

Midostaurin 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

查看 VEGFR 亚型特异性产品:

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

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nNOS iNOS eNOS

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

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)

细胞效力
(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]

体外研究
(In Vitro)

Midostaurin (PKC412) 在体外对各种肿瘤和正常细胞系表现出广泛的抗增殖活性，并且能够在体外逆转 Pgp 介导的肿瘤细胞多药耐药性。细胞暴露于 Midostaurin (PKC412) 会导致细胞周期的 G2/M 期剂量依赖性增加，同时多倍体增加、细胞凋亡和电离辐射敏感性增强^[1]。
Midostaurin (PKC412) 显著抑制 KIT-、Lyn-和 STAT5 活性，但不抑制 HMC-1 细胞和原发性肿瘤肥大细胞中的 Btk^[3]。
Midostaurin (PKC412) 抑制造血 Ba/F3 细胞中的 EN 融合酪氨酸激酶。Midostaurin (PKC412) 以剂量依赖性方式显著抑制 M0-91 和 IMS-M2 细胞中的 EN 磷酸化^[4]。

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

体内研究
(In Vivo)

Midostaurin (PKC412) 强烈抑制小鼠模型中的视网膜新生血管形成以及激光诱导的脉络膜新生血管形成^[1]。
Midostaurin (PKC412) (25 mg/kg，腹腔注射) 保护 K18 Arg90Cys 过表达转基因小鼠的小鼠肝脏免受 Fas 诱导的细胞凋亡^[5]。

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

Clinical Trial

分子量

570.64

Formula

C₃₅H₃₀N₄O₄

CAS 号

120685-11-2

性状

固体

颜色

White to yellow

中文名称

米哚妥林

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (87.62 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.38 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.38 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

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

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.91%

选择批次：

Data Sheet (659 KB) SDS (393 KB)

COA (299 KB) HNMR (274 KB) RP-HPLC (244 KB) LCMS (93 KB)

产品使用指南 (1538 KB)

参考文献

[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.
参考文献	[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]

Midostaurin 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

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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.

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Midostaurin (Synonyms: 米哚妥林; PKC412; CGP 41251)

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Midostaurin (Synonyms: 米哚妥林; PKC412; CGP 41251)

Customer Review

Other Forms of Midostaurin:

Midostaurin 相关抗体

MCE 顾客使用本产品发表的 26 篇科研文献

Midostaurin 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 PKC 亚型特异性产品:

查看 VEGFR 亚型特异性产品:

查看 NO Synthase 亚型特异性产品:

生物活性

实验参考方法

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Midostaurin 相关抗体:

摩尔计算器

稀释计算器

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