MLN8054

目錄號: HY-10180 純度: 99.54%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南

摩爾計算器

MLN8054是高效，選擇性，有口服活性的極光激酶 (aurora A) 抑制劑，IC₅₀ 值為4 nM。

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MLN8054 Chemical Structure

CAS No. : 869363-13-3

1. 客戶無需承擔(dān)相應(yīng)的運輸費用。

2. 同一機構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機構(gòu)（單位）一年內(nèi)

可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

3. 試用裝只面向終端客戶。

規(guī)格	價格	是否有貨
1 mg	￥454	In-stock
5 mg	￥1100	In-stock
10 mg	￥1600	In-stock
25 mg	￥3000	In-stock
50 mg	￥4800	In-stock
100 mg	現(xiàn)貨	詢價
200 mg		詢價
500 mg		詢價

or 大包裝詢價

* Please select Quantity before adding items.

Customer Review

Other Forms of MLN8054:

MLN8054 sodium 詢價

MCE 顧客使用本產(chǎn)品發(fā)表的 10 篇科研文獻

•Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. [Abstract]
•Cancer Res. 2017 Sep 15;77(18):4785-4796. [Abstract]
•PLoS Biol. 2020 Jun 9;18(6):e3000288. [Abstract]
•EMBO Rep. (2021)e51847.
•Comput Struct Biotechnol J. 2019 Feb 8;17:352-361. [Abstract]
•Anticancer Drugs. 2023 Jul 14. [Abstract]
•Patent. US20210299273A1.
•Technical University of Munich. 24.01.2018.
•J Biomol Screen. 2013 Oct;18(9):1062-71. [Abstract]
•Harvard Medical School LINCS LIBRARY

MLN8054 相關(guān)產(chǎn)品

•相關(guān)化合物庫:

•同靶點產(chǎn)品:

•同靶點蛋白產(chǎn)品:

查看 Aurora Kinase 亞型特異性產(chǎn)品:

查看所有亞型

Aurora Kinase Aurora A Aurora B Aurora C

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

MLN8054 is a potent, selective and orally available aurora A kinase inhibitor with an IC₅₀ of 4 nM.

IC₅₀ & Target

Aurora A

4 nM (IC₅₀)

細胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
Calu-6	IC₅₀	0.22 μM Compound: MLN-8054	Antiproliferative activity against human Calu6 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human Calu6 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
DLD-1	IC₅₀	1.43 μM Compound: MLN-8054	Antiproliferative activity against human DLD1 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human DLD1 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
HCT-116	IC₅₀	0.1 μM Compound: 1, MLN-8054	Antiproliferative activity against human HCT116 cells after 4 days by celltiter assay Antiproliferative activity against human HCT116 cells after 4 days by celltiter assay	[PMID: 19402633]
HCT-116	IC₅₀	0.16 μM Compound: 1, MLN-8054	Inhibition of Aurora A in human HCT116 cells assessed as complete failure of centrosome seperation by immunofluorescence assay Inhibition of Aurora A in human HCT116 cells assessed as complete failure of centrosome seperation by immunofluorescence assay	[PMID: 19402633]
HCT-116	IC₅₀	0.18 μM Compound: MLN-8054	Antiproliferative activity against human HCT116 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human HCT116 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
HCT-116	GI₅₀	0.22 μM Compound: 8, MLN8054	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	0.31 μM Compound: 1, MLN-8054	Inhibition of Aurora A in human HCT116 cells assessed as complete loss of phospho-Aurora A staining in centrosomes by immunofluorescence assay Inhibition of Aurora A in human HCT116 cells assessed as complete loss of phospho-Aurora A staining in centrosomes by immunofluorescence assay	[PMID: 19402633]
HCT-116	IC₅₀	0.69 μM Compound: MLN8054	Cytotoxicity against human HCT116 cells after 5 days by MTS assay Cytotoxicity against human HCT116 cells after 5 days by MTS assay	[PMID: 22326168]
HCT-116	IC₅₀	0.85 μM Compound: MLN8054	Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30143423]
HCT-116	IC₅₀	34 nM Compound: 8, MLN8054	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	34 nM Compound: 4, MLN-8054	Inhibition of aurora A autophosphorylation in human HCT116 cells by immunofluorescence method Inhibition of aurora A autophosphorylation in human HCT116 cells by immunofluorescence method	[PMID: 19320489]
HCT-116	IC₅₀	4 μM Compound: 4, MLN-8054	Inhibition of aurora B in human HCT116 cells assessed as inhibition of histone H3 Ser10 phosphorylation by immunofluorescence method Inhibition of aurora B in human HCT116 cells assessed as inhibition of histone H3 Ser10 phosphorylation by immunofluorescence method	[PMID: 19320489]
HCT-116	IC₅₀	5 μM Compound: 1, MLN-8054	Inhibition of Aurora B in human HCT116 cells assessed as complete loss of phospho-histamine H3 staining by immunofluorescence assay Inhibition of Aurora B in human HCT116 cells assessed as complete loss of phospho-histamine H3 staining by immunofluorescence assay	[PMID: 19402633]
HCT-116	IC₅₀	5.2 μM Compound: 8, MLN8054	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]
HeLa	IC₅₀	0.034 μM Compound: MLN-8054	Inhibition of Aurora A Thr288 autophosphorylation in human HeLa cells after 1 hr Inhibition of Aurora A Thr288 autophosphorylation in human HeLa cells after 1 hr	[PMID: 17360485]
HeLa	IC₅₀	5.7 μM Compound: MLN-8054	Inhibition of Aurora B Ser10 phosphorylation in human HeLa cells after 1 hr Inhibition of Aurora B Ser10 phosphorylation in human HeLa cells after 1 hr	[PMID: 17360485]
HT-29	IC₅₀	0.15 μM Compound: 1, MLN-8054	Antiproliferative activity against human HT-29 cells after 4 days by celltiter assay Antiproliferative activity against human HT-29 cells after 4 days by celltiter assay	[PMID: 19402633]
MCF7	IC₅₀	0.67 μM Compound: MLN-8054	Antiproliferative activity against human MCF7 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human MCF7 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
MDA-MB-231	IC₅₀	0.74 μM Compound: MLN-8054	Antiproliferative activity against human MDAMB231 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human MDAMB231 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
NCI-H460	IC₅₀	0.11 μM Compound: MLN-8054	Antiproliferative activity against human H460 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human H460 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
PC-3	IC₅₀	0.79 μM Compound: MLN-8054	Antiproliferative activity against human PC3 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human PC3 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
Sf9	IC₅₀	0.004 μM Compound: MLN-8054	Inhibition of mouse recombinant Aurora A kinase expressed in insect Sf9 cells by radioactive flashplate assay Inhibition of mouse recombinant Aurora A kinase expressed in insect Sf9 cells by radioactive flashplate assay	[PMID: 17360485]
Sf9	IC₅₀	0.172 μM Compound: MLN-8054	Inhibition of mouse recombinant Aurora B kinase expressed in insect Sf9 cells by radioactive flashplate assay Inhibition of mouse recombinant Aurora B kinase expressed in insect Sf9 cells by radioactive flashplate assay	[PMID: 17360485]
Sf9	IC₅₀	172 nM Compound: MLN8054	Inhibition of GST-tagged recombinant mouse Aurora B expressed in Sf9 cells using Biotin-TKQTARKSTGGKAPR as peptide substrate by [gamma-33S]ATP binding assay Inhibition of GST-tagged recombinant mouse Aurora B expressed in Sf9 cells using Biotin-TKQTARKSTGGKAPR as peptide substrate by [gamma-33S]ATP binding assay	[PMID: 24681066]
Sf9	IC₅₀	172 nM Compound: MLN8054	Inhibition of mouse recombinant Aurora B expressed in Sf9 cells using Biotin-TKQTARKSTGGKAPR as substrate and [gamma33P]ATP by flashplate assay Inhibition of mouse recombinant Aurora B expressed in Sf9 cells using Biotin-TKQTARKSTGGKAPR as substrate and [gamma33P]ATP by flashplate assay	[PMID: 22803810]
Sf9	IC₅₀	31 nM Compound: 8, MLN8054	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]
Sf9	IC₅₀	4 nM Compound: MLN8054	Inhibition of recombinant mouse Aurora A kinase expressed in Sf9 cells using Biotin-GLRRASLG as substrate in presence of [gamma33]P-ATP by FlashPlate assay Inhibition of recombinant mouse Aurora A kinase expressed in Sf9 cells using Biotin-GLRRASLG as substrate in presence of [gamma33]P-ATP by FlashPlate assay	[PMID: 30502115]
Sf9	IC₅₀	4 nM Compound: MLN8054	Inhibition of GST-tagged recombinant mouse Aurora A expressed in Sf9 cells using biotin-GLRRASLG as peptide substrate by [gamma-33S]ATP binding assay Inhibition of GST-tagged recombinant mouse Aurora A expressed in Sf9 cells using biotin-GLRRASLG as peptide substrate by [gamma-33S]ATP binding assay	[PMID: 24681066]
Sf9	IC₅₀	4 nM Compound: MLN8054	Inhibition of mouse recombinant Aurora A expressed in Sf9 cells using Biotin-GLRRASLG as substrate and [gamma33P]ATP by flashplate assay Inhibition of mouse recombinant Aurora A expressed in Sf9 cells using Biotin-GLRRASLG as substrate and [gamma33P]ATP by flashplate assay	[PMID: 22803810]
SK-OV-3	IC₅₀	0.53 μM Compound: MLN-8054	Antiproliferative activity against human SKOV3 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human SKOV3 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]
SW480	IC₅₀	0.86 μM Compound: MLN-8054	Antiproliferative activity against human SW480 cells after 96 hrs by BrdU cell proliferation ELISA Antiproliferative activity against human SW480 cells after 96 hrs by BrdU cell proliferation ELISA	[PMID: 17360485]

體外研究
(In Vitro)

MLN8054 is an ATP-competitive, reversible inhibitor of recombinant Aurora A kinase. MLN8054 is >40-fold more selective for Aurora A compared with the family member Aurora B. MLN8054 selectively inhibits Aurora A over Aurora B in cultured human tumor cells. MLN8054 treatment results in G2/M accumulation and spindle defects and inhibits proliferation in multiple cultured human tumor cells lines. MLN8054 effectively inhibits the growth of cells from diverse tissue origins with IC₅₀ values ranging from 0.11 to 1.43 μM^[1]. Treatment of human tumor cells grown in culture with MLN8054 shows a number of morphologic and biochemical changes associated with senescence^[2].

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

體內(nèi)研究
(In Vivo)

In the HCT-116 tumor-bearing mice, MLN8054 treatment inhibits tumor growth dose dependently. MLN8054 is generally well tolerated. MLN8054 also inhibits the growth of the PC-3 tumor xenograft in nude mice. MLN8054 Treatment Results in Inhibition of Aurora A, Accumulation of Mitotic Cells, and Apoptosis in vivo^[1]. MLN8054 selectively inhibits Aurora A kinase activity when dosed at 30 mg/kg. At this dose in HCT116 tumor tissue, MLN8054 has been shown to inhibit Aurora A autophosphorylation, and induce an increase in the Aurora B substrate, pHisH3^[2].

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

Clinical Trial

分子量

476.86

Formula

C₂₅H₁₅ClF₂N₄O₂

CAS 號

869363-13-3

性狀

固體

顏色

White to 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	1 year
	-20°C	6 months

溶解性數(shù)據(jù)

細胞實驗：

DMSO 中的溶解度 : 20.83 mg/mL (43.68 mM; 超聲助溶 (<60°C); 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	2.0971 mL	10.4853 mL	20.9705 mL
5 mM	0.4194 mL	2.0971 mL	4.1941 mL
10 mM	0.2097 mL	1.0485 mL	2.0971 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, 1 year; -20°C, 6 months。-80°C儲存時，請在1年內(nèi)使用， -20°C儲存時，請在6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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

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 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.24 mM); 懸濁液; 超聲助溶

此方案可獲得 2.5 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 25.0 mg/mL 的澄清 DMSO 儲備液加到 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。
方案二

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.36 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 20.8 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。
方案三

請依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.36 mM); 澄清溶液

此方案可獲得 ≥ 2.08 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 20.8 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

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）。

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: 99.54%

選擇批次：

Data Sheet (635 KB) SDS (251 KB)

COA (205 KB) LCMS (267 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻

[1]. Manfredi MG, et al. Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. Proc Natl Acad Sci U S A. 2007 Mar 6;104(10):4106-11. [Content Brief]

[2]. Huck JJ, et al. MLN8054, an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo. Mol Cancer Res. 2010 Mar;8(3):373-84. [Content Brief]

Cell Assay ^[1]	MLN8054 is added to human tumor cells in 2-fold serial dilutions to achieve final concentrations ranging from 10 to 0.04 mM. MLN8054 at each dilution is added in triplicate with each replicate on a separate plate. Cells treated with DMSO (n=6 wells per plate; 0.2% final concentration) served as the untreated control. The cells are treated with MLN8054 for 96 h at 37°C in a humidified cell culture chamber. Cell viability in each cell line is measured by using the Cell Proliferation ELISA, BrdU colorimetric kit^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: Nude mice bearing HCT-116 tumors are treated orally once per day for 21 consecutive days with either vehicle control or MLN8054 at doses of 3, 10, or 30 mg/kg. Tumor volumes are measured by using a vernier caliper and calculated^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻	[1]. Manfredi MG, et al. Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. Proc Natl Acad Sci U S A. 2007 Mar 6;104(10):4106-11. [Content Brief] [2]. Huck JJ, et al. MLN8054, an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo. Mol Cancer Res. 2010 Mar;8(3):373-84. [Content Brief]

MLN8054 相關(guān)分類

完整儲備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0971 mL	10.4853 mL	20.9705 mL	52.4263 mL
	5 mM	0.4194 mL	2.0971 mL	4.1941 mL	10.4853 mL
	10 mM	0.2097 mL	1.0485 mL	2.0971 mL	5.2426 mL
	15 mM	0.1398 mL	0.6990 mL	1.3980 mL	3.4951 mL
	20 mM	0.1049 mL	0.5243 mL	1.0485 mL	2.6213 mL
	25 mM	0.0839 mL	0.4194 mL	0.8388 mL	2.0971 mL
	30 mM	0.0699 mL	0.3495 mL	0.6990 mL	1.7475 mL
	40 mM	0.0524 mL	0.2621 mL	0.5243 mL	1.3107 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.

Keywords:

MLN8054869363-13-3MLN 8054MLN-8054Aurora KinaseInhibitorinhibitorinhibit

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MLN8054

Customer Review

Other Forms of MLN8054:

MCE 顧客使用本產(chǎn)品發(fā)表的 10 篇科研文獻

MLN8054 相關(guān)產(chǎn)品

•相關(guān)化合物庫:

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MLN8054

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MCE 顧客使用本產(chǎn)品發(fā)表的 10 篇科研文獻

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純度 & 產(chǎn)品資料

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MLN8054 相關(guān)抗體:

摩爾計算器

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