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  2. Metabolic Enzyme/Protease
  3. NEDD8-activating Enzyme
  4. Pevonedistat

Pevonedistat  (Synonyms: MLN4924)

目錄號: HY-70062 純度: 99.43%
COA 產品使用指南

Pevonedistat (MLN4924) 是一種有效，選擇性的NEDD8 活化酶 (NAE) 抑制劑，IC50 為 4.7 nM。

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Pevonedistat Chemical Structure

Pevonedistat Chemical Structure

CAS No. : 905579-51-3

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規(guī)格 價格 是否有貨 數量
10 mM * 1 mL in DMSO ￥1210
In-stock
1 mg ￥450
In-stock
5 mg ￥1100
In-stock
10 mg ￥1750
In-stock
50 mg ￥4500
In-stock
100 mg 現貨 詢價
200 mg   詢價  
500 mg   詢價  

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Customer Review

Other Forms of Pevonedistat:

MCE 顧客使用本產品發(fā)表的 145 篇科研文獻

WB
IF
IHC

    Pevonedistat purchased from MCE. Usage Cited in: Nat Microbiol. 2019 May;4(5):813-825.  [Abstract]

    293T cells are treated with MLN4924 and then co-transfected with PSGL-1 and Vpu or an empty vector. One day after the transfection, the cells are treated with CHX and collected at the indicated time points. The cell lysates are analysed by western blotting.

    Pevonedistat purchased from MCE. Usage Cited in: Nat Microbiol. 2019 May;4(5):813-825.  [Abstract]

    293T cells are treated with MLN4924 at the indicated concentrations 24 h before the cells are transfected with plasmids expressing PSGL-1 and Vpu. Two days after transfection, the cells are harvested and analysed by western blotting. Empty vector (–) was used as a negative control for the Vpu- or PSGL-1-expressing vectors.

    Pevonedistat purchased from MCE. Usage Cited in: Nat Plants. 2019 Jan;5(1):34-40.   [Abstract]

    Western analysis of LHCSR1 and LHCSR3 protein expression in the treatment of MLN4924 with different concentrations.

    Pevonedistat purchased from MCE. Usage Cited in: Lab Invest. 2019 Apr;99(4):528-538.  [Abstract]

    Western blot analysis of p65 phosphorylation in synovial cells induced by 100 ng/ml IL-17A with or without 100 nM MLN4924 pretreatment.

    Pevonedistat purchased from MCE. Usage Cited in: Am J Physiol Lung Cell Mol Physiol. 2019 Jun 1;316(6):L1070-L1080.  [Abstract]

    Immunoblotting analysis of degradation of IκBα, and levels of p-p65 (also known as RELA) and the NEDD8–Cullin compared with β-actin and total p65 in cell lysates from pulmonary epithelial cells stimulated with rmIL-17A (50 ng/ml) for 15 min after preincubation with the indicated concentration of MLN4924 (MLN) or DMSO for 0.5 h.

    Pevonedistat purchased from MCE. Usage Cited in: Am J Physiol Lung Cell Mol Physiol. 2019 Jun 1;316(6):L1070-L1080.  [Abstract]

    Immunoblotting analysis of p-p38, JNK, and ERK compared with total p38, JNK, and ERK in cell lysates from pulmonary epithelial cells stimulated as above.

    Pevonedistat purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2019 Jan 15;508(3):986-990.   [Abstract]

    MLN4924 antagonizes the suppressive effects of PTX on cytoskeletal organization in HO8910 and OVA-W cells. (A, C) After treatment with PTX and/or MLN4924 for 48 h, HO8910 and OVA-W cells are stained for α-tubulin and analyzed for intracellular distribution by confocal microscopy. Overlay of blue (nuclei) and red (a-tubulin) channels is shown. (B, D) Levels of α-tubulin protein are further confirmed by western blotting with b-actin as the loading control.

    Pevonedistat purchased from MCE. Usage Cited in: Nat Commun. 2018 Sep 18;9(1):3801.  [Abstract]

    Trophozoites (3D7) are subjected to the indicated treatment for 6?h before analysis of ubiquitinated proteins. Samples treated with MLN4924 are incubated for an additional 3?h prior to DHA treatment. Blots are representative of 3-4 independent experiments.

    Pevonedistat purchased from MCE. Usage Cited in: Elife. 2018 Aug 1;7:e38430.  [Abstract]

    Kelly cells are treated with increasing concentrations of Thal and co-treated with 5 μM Bortezonib, 5 μM MLN4924, 0.5 μM MLN7243, or DMSO as a control. Following 24 h incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.

    Pevonedistat purchased from MCE. Usage Cited in: Int J Med Sci. 2018 Apr 3;15(7):674-681.  [Abstract]

    NB4 cells are treated with MLN4924 (0, 20, 40 and 80 nM) for 0, 24, 48 and 72 hours, and the protein levels of cullin1 are detected by western blotting, with β-actin used as loading control.

    Pevonedistat purchased from MCE. Usage Cited in: Eur Rev Med Pharmacol Sci. 2018 Dec;22(23):8273-8280.  [Abstract]

    AGS cells are transfected with Flag-MRFAP1 for 30 hours and treated with or with 2 μM MLN4924 for additional 4 hours, cells are harvested and subjected to immunoprecipitation with Flag M2 beads and then detected with Western blot.

    Pevonedistat purchased from MCE. Usage Cited in: Eur Rev Med Pharmacol Sci. 2018 Dec;22(23):8273-8280.  [Abstract]

    AGS cells are transfected with increased dose of Flag-FBXW8 for 30 hours, 2 μM MLN4924 are added where indicate 4 hours before harvested. Western blot assay is performed with indicated antibodies.

    Pevonedistat purchased from MCE. Usage Cited in: Eur Rev Med Pharmacol Sci. 2018 Dec;22(23):8273-8280.  [Abstract]

    MRFAP1 KO AGS cells are treated with or without 2 μM MLN4924 for 24 hours, cells are harvested and subjected to Western blot with indicated antibodies.

    Pevonedistat purchased from MCE. Usage Cited in: Cancer Chemother Pharmacol. 2018 Jun;81(6):1083-1093.  [Abstract]

    786-0 and ACHN cells are treated with MLN4924 (0.5 μM or 1 μM).γ-H2AX is detected by immunoblotting analysis.

    Pevonedistat purchased from MCE. Usage Cited in: Oncotarget. 2017 Oct 12;8(57):97178-97186.  [Abstract]

    After 4 hours 1 μM MLN4924 treatment, lysates from 293T cells stably expressing either Flag or Flag-FBXW8 are immunoprecipitated with anti-FLAG M2 resin. Bound proteins are eluted with FLAG peptide, and all separated cell lysate components are resolved on 10% SDS-PAGE gel, stained by Coomassie Brilliant or subjected to immunoblotting with the indicated antibodies.

    Pevonedistat purchased from MCE. Usage Cited in: Oncotarget. 2017 Sep 23;8(49):86395-86409.  [Abstract]

    Immunofluorescence results, showing that ROC1, DCAF1, DDB1, and TET1 knockdown, and treatment with MLN4924 leads to the reduction of 5hmC levels in A2780 cells. A2780 cells transfected with siNC, siROC1, siDCAF1, siDDB1 or siTET1 and treatment with MLN4924 are subjected to immunofluorescence analysis with antibodies to the indicated protein.

    Pevonedistat purchased from MCE. Usage Cited in: Elife. 2016 Apr 11;5:e14087.  [Abstract]

    Fbxo21-/- RAW264.7 cells are transfected with indicated amounts (0, 1 or 5 μg) Fbxo21-Myc and equal amounts of K29O-Ub-HA vectors for 48 hr, and then infected with VSV (MOI = 1) or HSV-1 (MOI = 5) for 2 hr in the presence or absence of MLN-4924 (10 nM). Then polyubiquitinated ASK1 is examined by immunoblot (IB) against HA after immuneprecipitations (IP).

    Pevonedistat purchased from MCE. Usage Cited in: Technol Cancer Res Treat. 2016 Aug;15(4):527-34.  [Abstract]

    MLN4924 induces accumulation of SCF E3 ligase substrates. Subconfluent cells are treated with MLN4924 (50 nM) or radiation (6 Gy) alone or in combination for 24 hours, followed by immunoblotting (IB) analysis using indicated antibodies.

    Pevonedistat purchased from MCE. Usage Cited in: Oncotarget. 2016 Oct 4;7(40):66087-66099.  [Abstract]

    MLN4924 increases the stability of RORα. MLN4924 increases the half-life of RORα. U2OS cells are transiently transfected with plasmids expressing the Flag-RORα. At 24 h after transfection, MLN4924 (1 μM) or DMSO are added into respective cell culture media. 24 h later, cells are treated with Cycloheximide (CHX) for 0, 3, 6, 4, 9 and 12 h. Equal amounts of whole cell lysates are analyzed by Western blot with a Flag antibody (M2). Actin is used as an internal control.

    Pevonedistat purchased from MCE. Usage Cited in: Oncotarget. 2016 Jun 14;7(24):35643-35654.  [Abstract]

    MLN4924 induces apoptosis is caspase dependent. BMDCs are cultured with MLN4924. Total cellular protein extracts are prepared and subjected to immunoblotting by using A. anti-PARP, anti-caspase-3, anti-caspase-7 antibodies and B. anti-cleaved PARP, anti-cleaved-caspase-3, anti-cleaved-caspase-7 antibodies. C. Caspase-3 activity is examined by caspase activity kit. D. Immunoblotting analysis is performed for erk, p-erk, cyclin D1 and cyclin D3 expression.

    Pevonedistat purchased from MCE. Usage Cited in: Ann Hematol. 2014 Sep;93(9):1499-508.  [Abstract]

    MLN4924-induced p21 high expression eliminates the cell cycle promotion effect of BM-MSCs on Reh cells. a Western blot analysis of p21, skp2, and bax expression in Reh cells treated by different concentration of MLN4924. b Under the treatment of 25 nM IDA, western blot analysis of p21 and skp2 expressions in Reh cells cultured with or without BM-MSCs in the presence of different concentrations of MLN4924 (0, 300, 700 nM). c Under the treatment of 250 nM VP16, western blot analysis of p21 and skp

    • 生物活性

    • 實驗參考方法

    • 純度 & 產品資料

    • 參考文獻

    生物活性

    Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM[1].

    IC50 & Target

    IC50: 4.7 nM (NAE)[1]
    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    0.63 μM
    Compound: MLN4924
    Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK-8 assay
    Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK-8 assay
    		[PMID: 33129593]
    A549 IC50
    47.79 μM
    Compound: MLN4924
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    		[PMID: 34624825]
    BEAS-2B IC50
    1.22 μM
    Compound: MLN4924
    Cytotoxicity against human BEAS-2B cells incubated for 48 hrs by CCK-8 assay
    Cytotoxicity against human BEAS-2B cells incubated for 48 hrs by CCK-8 assay
    		[PMID: 33129593]
    Caco-2 IC50
    4.4 μM
    Compound: MLN4924
    Cytotoxicity against human Caco2 cells after 72 hrs by MTT assay
    Cytotoxicity against human Caco2 cells after 72 hrs by MTT assay
    		[PMID: 29232579]
    CAPAN-1 IC50
    101 nM
    Compound: 1; MLN4924
    Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    		[PMID: 33857374]
    DU-145 IC50
    201 nM
    Compound: 1; MLN4924
    Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    		[PMID: 33857374]
    EKVX IC50
    > 10 μM
    Compound: MLN4924
    Antiproliferative activity against human EKVX cells measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human EKVX cells measured after 48 hrs by CCK8 assay
    		[PMID: 31732254]
    EKVX IC50
    0.3 μM
    Compound: MLN4924
    Antiproliferative activity against human EKVX cells measured after 72 to 96 hrs by CCK8 assay
    Antiproliferative activity against human EKVX cells measured after 72 to 96 hrs by CCK8 assay
    		[PMID: 31732254]
    GES1 IC50
    13.45 μM
    Compound: MLN4924
    Cytotoxicity against human GES1 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Cytotoxicity against human GES1 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    		[PMID: 34624825]
    HCT-116 IC50
    0.19 μM
    Compound: MLN4924
    Antitumor activity against human HCT116 cells after 72 hrs by MTT assay
    Antitumor activity against human HCT116 cells after 72 hrs by MTT assay
    		[PMID: 28388520]
    HCT-116 IC50
    33.89 nM
    Compound: 1; MLN4924
    Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition by sulforhodamine B assay
    Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition by sulforhodamine B assay
    		[PMID: 33857374]
    HCT-116 IC50
    36.2 nM
    Compound: 1; MLN4924
    Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    		[PMID: 33857374]
    HepG2 IC50
    > 10 μM
    Compound: MLN4924
    Antiproliferative activity against human HepG2 cells measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human HepG2 cells measured after 48 hrs by CCK8 assay
    		[PMID: 31732254]
    HepG2 IC50
    0.3 μM
    Compound: MLN4924
    Antiproliferative activity against human HepG2 cells measured after 72 to 96 hrs by CCK8 assay
    Antiproliferative activity against human HepG2 cells measured after 72 to 96 hrs by CCK8 assay
    		[PMID: 31732254]
    HepG2 IC50
    8.15 μM
    Compound: MLN4924
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    		[PMID: 34624825]
    HGC-27 IC50
    1.25 μM
    Compound: MLN4924
    Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    		[PMID: 34624825]
    HT-29 IC50
    484 nM
    Compound: 1; MLN4924
    Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    		[PMID: 33857374]
    Huh-7 IC50
    > 10 μM
    Compound: MLN4924
    Antiproliferative activity against human HuH7 cells measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human HuH7 cells measured after 48 hrs by CCK8 assay
    		[PMID: 31732254]
    Huh-7 IC50
    0.3 μM
    Compound: MLN4924
    Antiproliferative activity against human HuH7 cells measured after 72 to 96 hrs by CCK8 assay
    Antiproliferative activity against human HuH7 cells measured after 72 to 96 hrs by CCK8 assay
    		[PMID: 31732254]
    HuTu80 IC50
    42.6 nM
    Compound: 1; MLN4924
    Antiproliferative activity against human HuTu80 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    Antiproliferative activity against human HuTu80 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    		[PMID: 33857374]
    Jurkat IC50
    152 nM
    Compound: 1; MLN4924
    Antiproliferative activity against human Jurkat cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    Antiproliferative activity against human Jurkat cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    		[PMID: 33857374]
    K562 EC50
    108 nM
    Compound: 2, MLN4924
    Antiproliferative activity against human K562 cells after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human K562 cells after 72 hrs by CellTiter-Glo assay
    		[PMID: 24900352]
    LNCaP-Clone-FGC IC50
    64.6 nM
    Compound: 1; MLN4924
    Antiproliferative activity against human LNCaP-Clone-FGC cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    Antiproliferative activity against human LNCaP-Clone-FGC cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    		[PMID: 33857374]
    MCF7 IC50
    > 10 μM
    Compound: MLN4924
    Antiproliferative activity against human MCF7 cells measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human MCF7 cells measured after 48 hrs by CCK8 assay
    		[PMID: 31732254]
    MCF7 IC50
    > 100 μM
    Compound: MLN4924
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    		[PMID: 34624825]
    MCF7 IC50
    0.3 μM
    Compound: MLN4924
    Antiproliferative activity against human MCF7 cells measured after 72 to 96 hrs by CCK8 assay
    Antiproliferative activity against human MCF7 cells measured after 72 to 96 hrs by CCK8 assay
    		[PMID: 31732254]
    MGC-803 IC50
    > 10 μM
    Compound: MLN4924
    Antiproliferative activity against human MGC803 cells measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human MGC803 cells measured after 48 hrs by CCK8 assay
    		[PMID: 31732254]
    MGC-803 IC50
    0.3 μM
    Compound: MLN4924
    Antiproliferative activity against human MGC803 cells measured after 72 to 96 hrs by CCK8 assay
    Antiproliferative activity against human MGC803 cells measured after 72 to 96 hrs by CCK8 assay
    		[PMID: 31732254]
    MGC-803 IC50
    5.16 μM
    Compound: MLN4924
    Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    		[PMID: 34624825]
    MKN-45 IC50
    > 10 μM
    Compound: MLN4924
    Antiproliferative activity against human MKN45 cells measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human MKN45 cells measured after 48 hrs by CCK8 assay
    		[PMID: 31732254]
    MKN-45 IC50
    0.3 μM
    Compound: MLN4924
    Antiproliferative activity against human MKN45 cells measured after 72 to 96 hrs by CCK8 assay
    Antiproliferative activity against human MKN45 cells measured after 72 to 96 hrs by CCK8 assay
    		[PMID: 31732254]
    MV4-11 IC50
    107 nM
    Compound: 1; MLN4924
    Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    		[PMID: 33857374]
    NCI-H1299 IC50
    > 10 μM
    Compound: MLN4924
    Antiproliferative activity against human H1299 cells measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human H1299 cells measured after 48 hrs by CCK8 assay
    		[PMID: 31732254]
    NCI-H1299 IC50
    0.3 μM
    Compound: MLN4924
    Antiproliferative activity against human H1299 cells measured after 72 to 96 hrs by CCK8 assay
    Antiproliferative activity against human H1299 cells measured after 72 to 96 hrs by CCK8 assay
    		[PMID: 31732254]
    NCI-H1299 IC50
    0.49 μM
    Compound: MLN4924
    Antiproliferative activity against human H1299 cells incubated for 48 hrs by CCK-8 assay
    Antiproliferative activity against human H1299 cells incubated for 48 hrs by CCK-8 assay
    		[PMID: 33129593]
    PLC IC50
    > 10 μM
    Compound: MLN4924
    Antiproliferative activity against human PLC cells measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human PLC cells measured after 48 hrs by CCK8 assay
    		[PMID: 31732254]
    PLC IC50
    0.3 μM
    Compound: MLN4924
    Antiproliferative activity against human PLC cells measured after 72 to 96 hrs by CCK8 assay
    Antiproliferative activity against human PLC cells measured after 72 to 96 hrs by CCK8 assay
    		[PMID: 31732254]
    RKO IC50
    166 nM
    Compound: 1; MLN4924
    Antiproliferative activity against human RKO cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    Antiproliferative activity against human RKO cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    		[PMID: 33857374]
    T47D IC50
    > 10 μM
    Compound: MLN4924
    Antiproliferative activity against human T47D cells measured after 48 hrs by CCK8 assay
    Antiproliferative activity against human T47D cells measured after 48 hrs by CCK8 assay
    		[PMID: 31732254]
    T47D IC50
    0.3 μM
    Compound: MLN4924
    Antiproliferative activity against human T47D cells measured after 72 to 96 hrs by CCK8 assay
    Antiproliferative activity against human T47D cells measured after 72 to 96 hrs by CCK8 assay
    		[PMID: 31732254]
    THP-1 IC50
    115 nM
    Compound: 1; MLN4924
    Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay
    		[PMID: 33857374]
    U2OS IC50
    0.16 μM
    Compound: MLN4924
    Antitumor activity against human U2OS cells after 72 hrs by MTT assay
    Antitumor activity against human U2OS cells after 72 hrs by MTT assay
    		[PMID: 28388520]
    體外研究
    (In Vitro)

    Pevonedistat (MLN4924) 是一種強效的 NAE 抑制劑，在監(jiān)測 E2-UBL 硫酯反應產物形成的純化酶測定中評估，相對于密切相關的酶 UAE、SAE、UBA6 和 ATG7（IC50 分別為 1.5、8.2、1.8 和 >10 μM）具有選擇性。在純化酶和細胞測定中，與密切相關的泛素活化酶 (UAE，也稱為 UBA1) 和 SUMO 活化酶 (SAE；SAE1 和 UBA2 亞基的異二聚體) 相比，Pevonedistat (MLN4924) 選擇性抑制 NAE 活性。MLN4924 對多種人類腫瘤衍生細胞系表現出強效的細胞毒活性[1]。

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

    Pevonedistat (MLN4924) (sc，10 mg/kg、30 mg/kg 或 60 mg/kg) 可抑制 NEDD8 通路，導致攜帶 HCT-116 異種移植瘤的小鼠出現 DNA 損傷[1]。
    Pevonedistat (sc，120 mg/kg) 和 TNF-α (10 μg/kg) 會協同引起 SD 大鼠的肝損傷[2]。

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

    443.52

    Formula

    C21H25N5O4S
    CAS 號
    性狀

    固體

    顏色

    White to light yellow

    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數據
    細胞實驗： 

    DMSO 中的溶解度 : 62.5 mg/mL (140.92 mM; 超聲助溶; 吸濕的 DMSO 對產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 質量 1 mg 5 mg 10 mg
    1 mM 2.2547 mL 11.2734 mL 22.5469 mL
    5 mM 0.4509 mL 2.2547 mL 4.5094 mL
    查看完整儲備液配制表

    * 請根據產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，避免反復凍融造成的產品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內使用， -20°C儲存時，請在1年內使用。

    • 摩爾計算器

    • 稀釋計算器

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

    質量
    =
    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：

    請根據您的 實驗動物和給藥方式 選擇適當的溶解方案。

    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：
    ——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議您現用現配，當天使用；
    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沉淀、析出現象，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    90% Saline

      Solubility: 5 mg/mL (11.27 mM); 懸濁液; 超聲助溶

    • 方案 二

      請依序添加每種溶劑： 5% DMSO    95% Saline

      Solubility: 2.5 mg/mL (5.64 mM); 懸濁液; 超聲助溶

    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 網站選購。 ，Tween 80，均可在 MCE 網站選購。
    計算結果
    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）。
    您所需的儲備液濃度超過該產品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術支持聯系。
    動物實驗體內工作液的配制方法 : 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 & 產品資料

    純度: 99.98%

    參考文獻
    Cell Assay
    [1]

    HCT-116 cells grown in 6-well cell-culture dishes are treated with 0.1% DMSO (control) or 0.3 μM Pevonedistat (MLN4924) for 24 h. Whole cell extracts are prepared and analysed by immunoblotting. For analysis of the E2-UBL thioester levels, lysates are fractionated by non-reducing SDS-PAGE and immunoblotted with polyclonal antibodies to Ubc12, Ubc9 and Ubc10. For analysis of other proteins, lysates are fractionated by reducing SDS-PAGE and probed with primary antibodies as follows: mouse monoclonal antibodies to CDT1, p27, geminin, ubiquitin, securin/PTTG and p53 or rabbit polyclonal antibodies to NRF2, Cyclin B1 and GADD34[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][2]

    Mice[1]
    Mice bearing HCT-116 tumours of 300-500 mm3 are administered a single Pevonedistat (MLN4924) dose (of 10, 30 or 60 mg/kg), and tumors are excised at various time-points over the subsequent 24 h period. The relative levels of NEDD8-cullin and NRF2 are estimated by quantitative immunoblot analysis using Alexa680-labelled anti-IgG as the secondary antibody. The statistical difference between the groups for NEDD8-cullin inhibition is determined using the Kruskal-Wallis test. For the analysis of CDT1 and phosphorylated CHK1 (Ser317) levels in tumour sections, formalin-fixed, paraffin-embedded tumour sections are stained with the relevant antibodies, amplified with HRP-labelled secondary antibodies and detected with the ChromoMap DAB Kit. Slides are counterstained with haematoxylin. Images are captured using an Eclipse E800 microscope and Retiga EXi colour digital camera and processed using Metamorph software. CDT1 and phosphorylated CHK1 levels are expressed as a function of the DAB signal area.
    Rats[2]
    Ten-week-old male Sprague-Dawley rats are used. Across two studies, a total of eight animals in each group are dosed with vehicle, TNF-α, Pevonedistat (MLN4924), or Pevonedistat (MLN4924)+TNF-α. Animals are first intravenously administered either vehicle (1×PBS) or 10 μg/kg TNF-α. One hour later, they are subcutaneously administered vehicle (20% sulfobutyl ether beta-cyclodextrin in 50 mM citrate buffer, pH 3.3) or 120 mg/kg Pevonedistat (MLN4924). Scheduled euthanasia occurred 24 h postdose. Unscheduled euthanasia is performed when animals exhibited moribund conditions. Serum is collected at necropsy and analyzed by Idexx Laboratories for serum chemistry markers of liver damage. Additionally, the livers from five animals in each group are removed, separated into two sections and either frozen at -80°C for subsequent protein analysis or fixed in 10% neutral buffered formalin, embedded in paraffin, sectioned at 4-6 μm, mounted on glass slides, stained with hematoxylin and eosin, and analyzed with an Olympus BX51 light microscope for histopathology assessment. Microscopic findings are recorded in concordance with the standardized nomenclature for classifying lesions within the livers of rats.

    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

    * 請根據產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，避免反復凍融造成的產品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內使用， -20°C儲存時，請在1年內使用。

    可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2547 mL 11.2734 mL 22.5469 mL 56.3672 mL
    5 mM 0.4509 mL 2.2547 mL 4.5094 mL 11.2734 mL
    10 mM 0.2255 mL 1.1273 mL 2.2547 mL 5.6367 mL
    15 mM 0.1503 mL 0.7516 mL 1.5031 mL 3.7578 mL
    20 mM 0.1127 mL 0.5637 mL 1.1273 mL 2.8184 mL
    25 mM 0.0902 mL 0.4509 mL 0.9019 mL 2.2547 mL
    30 mM 0.0752 mL 0.3758 mL 0.7516 mL 1.8789 mL
    40 mM 0.0564 mL 0.2818 mL 0.5637 mL 1.4092 mL
    50 mM 0.0451 mL 0.2255 mL 0.4509 mL 1.1273 mL
    60 mM 0.0376 mL 0.1879 mL 0.3758 mL 0.9395 mL
    80 mM 0.0282 mL 0.1409 mL 0.2818 mL 0.7046 mL
    100 mM 0.0225 mL 0.1127 mL 0.2255 mL 0.5637 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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    產品名稱：
    Pevonedistat
    目錄號：
    HY-70062
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