MLN0905
Based on 5 publication(s) in Google Scholar
MLN0905 is a potent, orally active Polo-like kinase 1 (PLK1) inhibitor. MLN0905 has inhibitory potency against PLK1 with an IC50 value of 2 nM. MLN0905 can be used for the research of cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.01%
- CAS 番号: 1228960-69-7
- 分子式: C24H25F3N6S
- 分子量:486.56
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Cell Imaging/Staining
生物活性
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PLK1 2 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HeLa | EC50 |
29 μM
Compound: 12c, MLN0905
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Inhibition of PLK-1 T210D mutant in human HeLa cells assessed as inhibition of Cdc25c phosphorylation at Thr-96 after 2 hrs by immunostaining
Inhibition of PLK-1 T210D mutant in human HeLa cells assessed as inhibition of Cdc25c phosphorylation at Thr-96 after 2 hrs by immunostaining
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[PMID: 22070629] |
MLN0905 (compound 12c) has inhibitory potency against PLK1 with an IC50 value of 2 nM[1].
MLN0905 exhibits potent activities for Cdc25C with an EC50 value of 33 nM[1].
MLN0905 shows inhibitory effects on HT29, HCT116, H460, and A375 cell lines with LD50 values of 22 nM, 56 nM, 89 nM and 34 nM, respectively[1].
MLN0905 (125 nM) shows strong mitotic arrest and monopolar spindle formation in HT-29 cells[1].
MLN0905 suppresses the growth of lymphoma cell lines with IC50 values ranging from 3 - 24 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MLN0905 (p.o.; 6.25, 12.5, 25, 50 mg/kg) exhibits significant antitumor activities in mice HT29 xenograft tumors[1].
MLN0905 (p.o.; 0-14.5 mg/kg; daily, QD×3/week) has marked antitumor effects in kinds of lymphoma xenograft model[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Tumor (HT29) xenograft model[1]
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Dosage:0-50 mg/kg
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Administration:P.O; daily, QD×3/week
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Result:Observed antitumor activity, tumor stasis or regression and well-tolerated oral doses.
化学情報
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CAS 番号 1228960-69-7
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性状 Solid
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分子量 486.56
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分子式 C24H25F3N6S
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Color Off-white to yellow
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SMILES
CC1=NC=C(CCCN(C)C)C=C1NC2=NC(C(C=CC(C(F)(F)F)=C3)=C3NC(C4)=S)=C4C=N2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Commun
RIOK2 kinase regulates the translocation of the FADD-RIPK1-Caspase-8 complex to the ER and the cleavage of Gasdermin D to drive pyroptosis. [Abstract]2025 Nov 17;16(1):10060. PMID: 41249793 -
Theranostics
Sequentially targeting and intervening mutual Polo-like Kinase 1 on CAFs and tumor cells by dual targeting nano-platform for cholangiocarcinoma treatment. [Abstract]2022 May 9;12(8):3911-3927. PMID: 35664077 -
Cell Death Dis
The E3 ligase TRIM26 suppresses ferroptosis through catalyzing K63-linked ubiquitination of GPX4 in glioma. [Abstract]2023 Oct 23;14(10):695. PMID: 37872147
MLN0905 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Oct 23;14(10):695. [Abstract]
PLA assay between TRIM26 and GPX4 in U118 cells treated with onvansertib (2 nM) or MLN0905 (2 nM).
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PLoS Negl Trop Dis
Structure-Bioactivity Relationship for Benzimidazole Thiophene Inhibitors of Polo-Like Kinase 1 (PLK1), a Potential Drug Target in Schistosoma mansoni. [Abstract]2016 Jan 11;10(1):e0004356. PMID: 26751972 -
溶剤 & 溶解度
DMSO : ≥ 30 mg/mL (61.66 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (282 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Duffey MO, et al. Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905). J Med Chem. 2012 Jan 12;55(1):197-208. [Content Brief]
[2]. Shi JQ, et al. MLN0905, a small-molecule plk1 inhibitor, induces antitumor responses in human models of diffuse large B-cell lymphoma. Mol Cancer Ther. 2012 Sep;11(9):2045-53. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0552 mL | 10.2762 mL | 20.5524 mL | 51.3811 mL |
| 5 mM | 0.4110 mL | 2.0552 mL | 4.1105 mL | 10.2762 mL | |
| 10 mM | 0.2055 mL | 1.0276 mL | 2.0552 mL | 5.1381 mL | |
| 15 mM | 0.1370 mL | 0.6851 mL | 1.3702 mL | 3.4254 mL | |
| 20 mM | 0.1028 mL | 0.5138 mL | 1.0276 mL | 2.5691 mL | |
| 25 mM | 0.0822 mL | 0.4110 mL | 0.8221 mL | 2.0552 mL | |
| 30 mM | 0.0685 mL | 0.3425 mL | 0.6851 mL | 1.7127 mL | |
| 40 mM | 0.0514 mL | 0.2569 mL | 0.5138 mL | 1.2845 mL | |
| 50 mM | 0.0411 mL | 0.2055 mL | 0.4110 mL | 1.0276 mL | |
| 60 mM | 0.0343 mL | 0.1713 mL | 0.3425 mL | 0.8564 mL |
MLN0905 関連分類
HY-15155 関連分類
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