ホームページ Cell Cycle Aurora Kinase inhibitor MLN8054 For research use only.

MLN8054

MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1.

MLN8054化学構造

CAS No. 869363-13-3

サイズ 価格(税別) 在庫状況
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JPY 48000 国内在庫あり
JPY 145500 国内在庫あり

代表番号: 045-509-1970|電子メール：[email protected]
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MLN8054関連製品

シグナル伝達経路

Aurora Kinase Signaling Pathways

Aurora Kinaseシグナル伝達経路

Aurora Kinase阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
human HeLa cells Function assay 1 h Inhibition of Aurora A Thr288 autophosphorylation in human HeLa cells after 1 hr, IC50=0.034 μM 17360485
human H460 cells Proliferation assay 96 h Antiproliferative activity against human H460 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=0.11 μM 17360485
human HT-29 cells Proliferation assay 4 days Antiproliferative activity against human HT-29 cells after 4 days by celltiter assay, IC50=0.15 μM 19402633
human Calu6 cells Proliferation assay 96 h Antiproliferative activity against human Calu6 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=0.22 μM 17360485
human SKOV3 cells Proliferation assay 96 h Antiproliferative activity against human SKOV3 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=0.53 μM 17360485
human MCF7 cells Proliferation assay 96 h Antiproliferative activity against human MCF7 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=0.67 μM 17360485
human MDAMB231 cells Proliferation assay 96 h Antiproliferative activity against human MDAMB231 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=0.74 μM 17360485
human PC3 cells Proliferation assay 96 h Antiproliferative activity against human PC3 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=0.79 μM 17360485
human SW480 cells Proliferation assay 96 h Antiproliferative activity against human SW480 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=0.86 μM 17360485
human DLD1 cells Proliferation assay 96 h Antiproliferative activity against human DLD1 cells after 96 hrs by BrdU cell proliferation ELISA, IC50=1.43 μM 17360485
DU-145 prostate cancer cell Function assay 96 h Inhibitory concentration against DU-145 prostate cancer cell proliferation over 96 hr, IC50=0.11 μM 16107152
Sf9 cells Function assay Inhibition of mouse recombinant Aurora A kinase expressed in insect Sf9 cells by radioactive flashplate assay, IC50=4 nM 17360485
human HCT116 cells Function assay Inhibition of aurora kinase A autophosphorylation at T288 in human HCT116 cells by immunofluorescence analysis, IC50=0.034 μM 26101564
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生物活性

製品説明 MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1.
Targets
Aurora A [1]
(Sf9 cells)		 Aurora B [1]
(Sf9 cells)
4 nM 172 nM
In Vitro
In vitro MLN8054 is an ATP-competitive, reversible inhibitor of recombinant Aurora A kinase with an IC50 of 4 nM, which shows >40-fold more selective inhibitory activity for Aurora A compared with Aurora B. [1] In vitro, MLN8054 exhibits the activity of growth inhibition across various cell lines from diverse tissue origins with IC50 values ranging from 0.11 μM to 1.43 μM. In addition, MLN8054 selectively inhibits Aurora A over Aurora B in cultured cells, and inhibits cell proliferation by promoting G2/M accumulation and spindle defects in multiple cultured human tumor cells lines. [1] A recent study shows that MLN8054 sensitizes androgen-resistant prostate cancer to radiation by inhibiting Aurora A kinase, which is associated with sustained DNA double-strand breaks. [2]
Kinase Assay Enzyme Assays
Recombinant murine Aurora A and Aurora B protein are expressed in Sf9 cells and purified with GST affinity chromatography. The peptide substrate for Aurora A is conjugated with biotin (Biotin-GLRRASLG). Aurora A kinase (5 nM) is assayed in 50 mM Hepes (pH 7.5)/10 mM MgCl2/5 mM DTT/0.05% Tween 20/2 μM peptide substrate/3.3 μCi/ml [γ-33P]ATP at 2 μM by using Image FlashPlates. Aurora B kinase (2 nM) is assayed with 10 μM biotinylated peptide Biotin-TKQTARKSTGGKAPR in 50 mM Tricine (pH 8.0)/2.5 mM MgCl2/5 mM DTT/10% glycerol/2% BSA/40 μCi/ml [γ-33P]ATP at 250 μM. The conditions for all other in vitro kinase assays are available upon request. MLN8054 is run in a 226 kinase screen at a 1 μM compound concentration with an ATP concentration of 10 μM for all assays.
細胞実験 細胞株 HCT-116, SW480, DLD-1, MCF-7, MDA-MB-231, Calu-6, H460, SKOV-3 and PC-3 cells
濃度 0.04-10 mM
反応時間 96 hours
実験の流れ Human tumor cell lines are grown in 96-well cell culture dishes according to the distributor's recommendations. MLN8054, diluted in DMSO, is added to the cells in 2-fold serial dilutions to achieve final concentrations ranging from 10 mM 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) serves as the untreated control. The cells are treated with MLN8054 for 96 hours 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 according to the manufacturer's recommendation
In Vivo
In Vivo In the HCT-116 tumor-bearing mice, MLN8054, administered orally at 3 mg/kg, 10 mg/kg, and 30 mg/kg once a day, leads to dose-dependent tumor growth inhibition (TGI: 76% and 84% for 10 mg/kg and 30 mg/kg). MLN8054 also shows similar antitumor activity in the PC-3 tumor xenograft in nude mice. [1] In the HCT-116 xenograft-bearing animals, MLN8054 induces DNA and tubulin staining of tumor tissue in nuclear and cell body area, consistent with a senescent phenotype by increasing senescence-associated beta-galactosidase activity. [3]
動物実験 動物モデル HCT-116 and PC-3 cells are injected s.c. into the right flank of nude mice.
投与量 ≤30 mg/kg
投与経路 Administered via p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00652158 Terminated
Advanced Malignancies
Millennium Pharmaceuticals Inc.
 April 2006 Phase 1
NCT00249301 Terminated
Breast Neoplasm|Colon Neoplasm|Pancreatic Neoplasm|Bladder Neoplasm
Millennium Pharmaceuticals Inc.
 October 2005 Phase 1

化学情報

分子量 476.86 化学式

C25H15ClF2N4O2
CAS No. 869363-13-3 SDF Download MLN8054 SDFをダウンロードする
Smiles C1C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)C(=N1)C4=C(C=CC=C4F)F)NC5=CC=C(C=C5)C(=O)O
保管

In vitro
Batch:

DMSO : 95 mg/mL ( (199.21 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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