Alisertib (Synonyms: MLN 8237)

目录号: HY-10971 纯度: 99.36%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Aliertib (MLN 8237) 是一种口服活性和选择性的 Aurora A 激酶抑制剂 (IC₅₀=1.2 nM)，与Aurora A 激酶结合，导致有丝分裂纺锤体异常、有丝分裂累积。Aliertib (MLN 8237) 通过靶向白血病细胞中的 AKT/mTOR/AMPK/p38 途径诱导其凋亡和自噬。具有抗肿瘤活性。

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Alisertib Chemical Structure

CAS No. : 1028486-01-2

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规格	价格	是否有货
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	现货	询价
500 mg	现货	询价
1 g		询价
5 g		询价

or 大包装询价

* Please select Quantity before adding items.

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Other Forms of Alisertib:

Alisertib sodium 询价

MCE 顾客使用本产品发表的 45 篇科研文献

IHC

: 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.

Alisertib 相关产品

•相关化合物库:

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查看所有亚型

Aurora Kinase Aurora A Aurora B Aurora C

生物活性
纯度 & 产品资料
参考文献

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)

细胞效力
(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]

体外研究
(In Vitro)

Alisertib (MLN 8237) 会导致多发性骨髓瘤（MM）细胞出现有丝分裂纺锤体异常、有丝分裂累积，并通过凋亡和衰老来抑制细胞增殖。 Alisertib 会上调 p53 和肿瘤抑制基因 p21 和 p27^[1]。
Alisertib (MLN 8237) 对 T217D/W277E Aurora A/TPX2 复合物的活性降低可能反映了辅因子与 Aurora A 结合引起的 ATP 亲和力增加^[2]。
Alisertib (MLN 8237) 抑制细胞增殖，在不同肿瘤细胞系中的 IC₅₀ 范围为 15 至 469 nM^[4]。

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

体内研究
(In Vivo)

Alisertib (MLN 8237) (30 mg/kg, p.o.) 显著降低人类 MM 异种移植小鼠模型中的肿瘤负担并提高总体生存率^[1]。
Alisertib（3-30 mg/kg; p.o.; 每天一次，持续 3 周）在实体瘤异种移植模型中可抑制肿瘤生长^[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 号

1028486-01-2

性状

固体

颜色

Light yellow to light pink

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : 25 mg/mL (48.18 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	1.9271 mL	9.6354 mL	19.2708 mL
5 mM	0.3854 mL	1.9271 mL	3.8542 mL
10 mM	0.1927 mL	0.9635 mL	1.9271 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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: 2.08 mg/mL (4.01 mM); 悬浊液; 超声助溶

此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 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% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.01 mM); 悬浊液; 超声助溶

此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.01 mM); 澄清溶液

此方案可获得 ≥ 2.08 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 20.8 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）。

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: 99.84%

选择批次：

Data Sheet (653 KB) SDS (393 KB)

COA (298 KB) HNMR (175 KB) LCMS (435 KB) 元素分析报告 (221 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Güllü G, et al. A novel Aurora-A kinase inhibitor MLN8237 induces cytotoxicity and cell-cycle arrest in multiple myeloma Blood June 24, 2010 vol. 115 no. 25 5202-5213. [Content Brief]

[2]. Sloane DA, et al. Drug-Resistant Aurora A Mutants for Cellular Target Validation of the Small Molecule Kinase Inhibitors MLN8054 and MLN8237 ACS Chem. Biol., 2010, 5 (6), pp 563-576. [Content Brief]

[3]. Bavetsias V, et al. Aurora Kinase Inhibitors: Current Status and Outlook. Front Oncol. 2015 Dec 21;5:278. [Content Brief]

[4]. Manfredi MG, et al. Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays.Clin Cancer Res. 2011 Dec 15;17(24):7614-7624. [Content Brief]

Alisertib 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	1.9271 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.

Keywords:

Alisertib1028486-01-2MLN 8237MLN8237MLN-8237Aurora KinaseAutophagyApoptosiscytotoxicitycell-cyclearrestmultiplemyelomamitoticspindlecancerInhibitorinhibitorinhibit

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Alisertib (Synonyms: MLN 8237)

Customer Review

Other Forms of Alisertib:

MCE 顾客使用本产品发表的 45 篇科研文献

Alisertib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Aurora Kinase 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

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Alisertib (Synonyms: MLN 8237)

Customer Review

Other Forms of Alisertib:

Alisertib 相关抗体

MCE 顾客使用本产品发表的 45 篇科研文献

Alisertib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Aurora Kinase 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

Alisertib 相关抗体:

摩尔计算器

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Alisertib 相关分类

完整储备液配制表

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