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

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

目錄號: HY-10230 純度: 99.91%
COA 產(chǎn)品使用指南 技術(shù)支持

Midostaurin (PKC412; CGP 41251) 是一種具有口服活性的可逆多靶點蛋白激酶抑制劑。Midostaurin 抑制 PKCα/β/γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ 和 VEGFR1/2，IC50 范圍為 22-500 nM。Midostaurin 還上調(diào)內(nèi)皮一氧化氮合酶 (eNOS) 基因表達。Midostaurin 顯示出強大的抗癌作用。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)

Midostaurin Chemical Structure

Midostaurin Chemical Structure

CAS No. : 120685-11-2

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規(guī)格 價格 是否有貨 數(shù)量
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 現(xiàn)貨 詢價
100 mg   詢價  
200 mg   詢價  

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Customer Review

Other Forms of Midostaurin:

    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.

    查看 PKC 亞型特異性產(chǎn)品:

    查看 VEGFR 亞型特異性產(chǎn)品:

    查看 NO Synthase 亞型特異性產(chǎn)品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    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)

    細(xì)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]
    體外研究
    (In Vitro)

    Midostaurin (PKC412) 在體外對各種腫瘤和正常細(xì)胞系表現(xiàn)出廣泛的抗增殖活性，并且能夠在體外逆轉(zhuǎn) Pgp 介導(dǎo)的腫瘤細(xì)胞多藥耐藥性。細(xì)胞暴露于 Midostaurin (PKC412) 會導(dǎo)致細(xì)胞周期的 G2/M 期劑量依賴性增加，同時多倍體增加、細(xì)胞凋亡和電離輻射敏感性增強[1]。
    Midostaurin (PKC412) 顯著抑制 KIT-、Lyn-和 STAT5 活性，但不抑制 HMC-1 細(xì)胞和原發(fā)性腫瘤肥大細(xì)胞中的 Btk[3]。
    Midostaurin (PKC412) 抑制造血 Ba/F3 細(xì)胞中的 EN 融合酪氨酸激酶。Midostaurin (PKC412) 以劑量依賴性方式顯著抑制 M0-91 和 IMS-M2 細(xì)胞中的 EN 磷酸化[4]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    Midostaurin (PKC412) 強烈抑制小鼠模型中的視網(wǎng)膜新生血管形成以及激光誘導(dǎo)的脈絡(luò)膜新生血管形成[1]。
    Midostaurin (PKC412) (25 mg/kg，腹腔注射) 保護 K18 Arg90Cys 過表達轉(zhuǎn)基因小鼠的小鼠肝臟免受 Fas 誘導(dǎo)的細(xì)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 號
    性狀

    固體

    顏色

    White to yellow

    中文名稱

    米哚妥林
    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式

    -20°C, sealed storage, away from moisture

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

    溶解性數(shù)據(jù)
    細(xì)胞實驗： 

    DMSO 中的溶解度 : 50 mg/mL (87.62 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.38 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請依序添加每種溶劑： 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.38 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

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

    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.91%

    參考文獻
    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.
    參考文獻

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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
    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.

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