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  2. Cell Cycle/DNA Damage Epigenetics Autophagy Apoptosis
  3. Aurora Kinase Autophagy Apoptosis
  4. Alisertib

Aliertib (MLN 8237) 是一種口服活性和選擇性的 Aurora A 激酶抑制劑 (IC50=1.2 nM)，與Aurora A 激酶結(jié)合，導(dǎo)致有絲分裂紡錘體異常、有絲分裂累積。Aliertib (MLN 8237) 通過靶向白血病細(xì)胞中的 AKT/mTOR/AMPK/p38 途徑誘導(dǎo)其凋亡和自噬。具有抗腫瘤活性。

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Alisertib Chemical Structure

Alisertib Chemical Structure

CAS No. : 1028486-01-2

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥799
In-stock
5 mg ￥700
In-stock
10 mg ￥980
In-stock
50 mg ￥2950
In-stock
100 mg ￥3850
In-stock
200 mg 現(xiàn)貨 詢價(jià)
500 mg 現(xiàn)貨 詢價(jià)
1 g   詢價(jià)  
5 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Alisertib:

MCE 顧客使用本產(chǎn)品發(fā)表的 49 篇科研文獻(xiàn)

IF
IHC
WB

    Alisertib purchased from MCE. Usage Cited in: FASEB J. 2018 May;32(5):2735-2746.  [Abstract]

    Representative immunofluorescence (IF) image and graph with frequency of ciliated WT or Pkd12/2 murine renal epithelial cells at 2 h after treatment with vehicle (V), Ganetespib (G), or Alisertib (A) to inhibit AURKA, or (C) combination of Alisertib and Ganetespib. On IF, acetylated a-tubulin (red); g-tubulin (green); DAPI (blue).

    Alisertib purchased from MCE. Usage Cited in: College of Medicine. Drexel University. 2016 Nov.

    Alisertib and combination treatment suppress proliferation in BT474 orthotopic tumors as shown by decrease in Ki-67, which is statistically significantly different between vehicle and combination treatment, FRAX1036 and Alisertib, and FRAX1036 and combination treatment.

    Alisertib purchased from MCE. Usage Cited in: College of Medicine. Drexel University. 2016 Nov.

    Alisertib enhances FRAX1036 inhibitory effect on PAK1 phosphorylation in BT474 xenograft model.

    查看 Aurora Kinase 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity[1][2][3].

    IC50 & Target[3]

    Aurora A

    1.2 nM (IC50)

    Aurora B

    396.5 nM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HCT-116 GI50
    0.03 μM
    Compound: 10, alisertib
    Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation by BrdU incorporation assay
    Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation by BrdU incorporation assay
    		[PMID: 26101564]
    HCT-116 IC50
    1.5 μM
    Compound: 10, alisertib
    Inhibition of aurora kinase B in human HCT116 cells assessed as inhibition of histone H3 phosphorylation by immunofluorescence analysis
    Inhibition of aurora kinase B in human HCT116 cells assessed as inhibition of histone H3 phosphorylation by immunofluorescence analysis
    		[PMID: 26101564]
    HCT-116 IC50
    32 μM
    Compound: MLN-8237
    Antiproliferative activity against human HCT116 cells measured after 96 hrs by Brdu incorporation-based ELISA
    Antiproliferative activity against human HCT116 cells measured after 96 hrs by Brdu incorporation-based ELISA
    		[PMID: 31381325]
    HCT-116 IC50
    7 nM
    Compound: 10, alisertib
    Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysis
    Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysis
    		[PMID: 26101564]
    HCT-116 IC50
    95 nM
    Compound: 29, MLN-8237
    Antiproliferative activity against human HCT116 cells after 72 hrs by WST8 assay
    Antiproliferative activity against human HCT116 cells after 72 hrs by WST8 assay
    		[PMID: 25625617]
    HCT-15 IC50
    740 nM
    Compound: 29, MLN-8237
    Antiproliferative activity against human HCT15 cells after 72 hrs by WST8 assay
    Antiproliferative activity against human HCT15 cells after 72 hrs by WST8 assay
    		[PMID: 25625617]
    HL-60 IC50
    74 nM
    Compound: 29, MLN-8237
    Antiproliferative activity against human HL60 cells after 72 hrs by WST8 assay
    Antiproliferative activity against human HL60 cells after 72 hrs by WST8 assay
    		[PMID: 25625617]
    HT-29 IC50
    330 nM
    Compound: 29, MLN-8237
    Antiproliferative activity against human HT-29 cells after 72 hrs by WST8 assay
    Antiproliferative activity against human HT-29 cells after 72 hrs by WST8 assay
    		[PMID: 25625617]
    LC-2-ad IC50
    77 nM
    Compound: 29, MLN-8237
    Antiproliferative activity against human LC2/ad cells after 72 hrs by WST8 assay
    Antiproliferative activity against human LC2/ad cells after 72 hrs by WST8 assay
    		[PMID: 25625617]
    LU-99A IC50
    62 nM
    Compound: 29, MLN-8237
    Antiproliferative activity against human LU99A cells after 72 hrs by WST8 assay
    Antiproliferative activity against human LU99A cells after 72 hrs by WST8 assay
    		[PMID: 25625617]
    MIA PaCa-2 IC50
    130 nM
    Compound: 29, MLN-8237
    Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by WST8 assay
    Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by WST8 assay
    		[PMID: 25625617]
    MKN-45 IC50
    93 nM
    Compound: 29, MLN-8237
    Antiproliferative activity against human MKN45 cells after 72 hrs by WST8 assay
    Antiproliferative activity against human MKN45 cells after 72 hrs by WST8 assay
    		[PMID: 25625617]
    MRC5 IC50
    > 10000 nM
    Compound: 29, MLN-8237
    Antiproliferative activity against human MRC5 cells after 72 hrs by WST8 assay
    Antiproliferative activity against human MRC5 cells after 72 hrs by WST8 assay
    		[PMID: 25625617]
    MV4-11 IC50
    1.2 nM
    Compound: 17
    Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation of cells at G2/M phase measured after 12 hrs
    Induction of cell cycle arrest in human MV4-11 cells assessed as accumulation of cells at G2/M phase measured after 12 hrs
    		[PMID: 36306471]
    NCI-H358 IC50
    100 nM
    Compound: 29, MLN-8237
    Antiproliferative activity against human NCI-H358 cells after 72 hrs by WST8 assay
    Antiproliferative activity against human NCI-H358 cells after 72 hrs by WST8 assay
    		[PMID: 25625617]
    PC-14 IC50
    170 nM
    Compound: 29, MLN-8237
    Antiproliferative activity against human PC14 cells after 72 hrs by WST8 assay
    Antiproliferative activity against human PC14 cells after 72 hrs by WST8 assay
    		[PMID: 25625617]
    Sf9 IC50
    1 nM
    Compound: 10, alisertib
    Inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells using biotin-GLRRASLG as substrate in presence of [gamma-33P]ATP
    Inhibition of recombinant mouse aurora kinase A expressed in insect Sf9 cells using biotin-GLRRASLG as substrate in presence of [gamma-33P]ATP
    		[PMID: 26101564]
    體外研究
    (In Vitro)

    Alisertib (MLN 8237) 會(huì)導(dǎo)致多發(fā)性骨髓瘤（MM）細(xì)胞出現(xiàn)有絲分裂紡錘體異常、有絲分裂累積，并通過凋亡和衰老來抑制細(xì)胞增殖。 Alisertib 會(huì)上調(diào) p53 和腫瘤抑制基因 p21 和 p27[1]。
    Alisertib (MLN 8237) 對(duì) T217D/W277E Aurora A/TPX2 復(fù)合物的活性降低可能反映了輔因子與 Aurora A 結(jié)合引起的 ATP 親和力增加[2]。
    Alisertib (MLN 8237) 抑制細(xì)胞增殖，在不同腫瘤細(xì)胞系中的 IC50 范圍為 15 至 469 nM[4]。

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

    Alisertib (MLN 8237) (30 mg/kg, p.o.) 顯著降低人類 MM 異種移植小鼠模型中的腫瘤負(fù)擔(dān)并提高總體生存率[1]。
    Alisertib（3-30 mg/kg; p.o.; 每天一次，持續(xù) 3 周）在實(shí)體瘤異種移植模型中可抑制腫瘤生長(zhǎng)[4]。

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

    Animal Model: Nude mice bearing HCT-116 colon tumor xenograft[4]
    Dosage: 3, 10, or 30 mg/kg
    Administration: P.o.; once daily for 3 weeks
    Result: Resulted in a dose-dependent TGI (tumor growth inhibition) of 43.3%, 84.2%, and 94.7% for the 3, 10, and 30 mg/kg groups,respectively.
    Clinical Trial
    分子量

    518.92

    Formula

    C27H20ClFN4O4
    CAS 號(hào)
    性狀

    固體

    顏色

    Light yellow to light pink

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 25 mg/mL (48.18 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.9271 mL 9.6354 mL 19.2708 mL
    5 mM 0.3854 mL 1.9271 mL 3.8542 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)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(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)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(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (4.01 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (4.01 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)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(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)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(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)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: 99.84%

    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)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 1.9271 mL 9.6354 mL 19.2708 mL 48.1770 mL
    5 mM 0.3854 mL 1.9271 mL 3.8542 mL 9.6354 mL
    10 mM 0.1927 mL 0.9635 mL 1.9271 mL 4.8177 mL
    15 mM 0.1285 mL 0.6424 mL 1.2847 mL 3.2118 mL
    20 mM 0.0964 mL 0.4818 mL 0.9635 mL 2.4088 mL
    25 mM 0.0771 mL 0.3854 mL 0.7708 mL 1.9271 mL
    30 mM 0.0642 mL 0.3212 mL 0.6424 mL 1.6059 mL
    40 mM 0.0482 mL 0.2409 mL 0.4818 mL 1.2044 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(chǎn)品名稱：
    Alisertib
    目錄號(hào)：
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