Ro3280
Based on 4 publication(s) in Google Scholar
Ro3280 is a potent, highly selective inhibitor of PLK1 with an IC50 and a Kd of 3 nM and 0.09 nM, respectively, and nearly has no effect on PLK2 and PLK3.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.46%
- No. CAS: 1062243-51-9
- Fòrmula: C27H35F2N7O3
- Peso molecular:543.61
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Ro3280
More
Customer Validation & Images
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Apoptosis Analysis
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Cell Imaging/Staining
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Flow Cytometry
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RT-PCR
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WB
Actividad biológica
Descripciòn
IC50 & Target
[2]|
PLK1 0.09 nM (Kd) |
ALK 230 nM (Kd) |
CAMKK1 1100 nM (Kd) |
CAMKK2 87 nM (Kd) |
DAPK1 100 nM (Kd) |
DAPK3 70 nM (Kd) |
FER 53 nM (Kd) |
GAK 87 nM (Kd) |
MYLK 170 nM (Kd) |
PTK2 84 nM (Kd) |
PTK2B 130 nM (Kd) |
RPS6KA6 (KinDom.2) 560 nM (Kd) |
TTK 51 nM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
2.6 nM
Compound: Ro3280
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Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay
Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay
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[PMID: 34710325] |
| HT-29 | EC50 |
5 nM
Compound: 11
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Antiproliferative activity against human HT-29 cells after 72 hrs by Cell Titer-Glo Assay
Antiproliferative activity against human HT-29 cells after 72 hrs by Cell Titer-Glo Assay
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[PMID: 23664874] |
| MM1.S | IC50 |
5.7 nM
Compound: Ro3280
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Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay
Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay
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[PMID: 34710325] |
In Vitro
Ro3280 (RO3280) inhibits PLK1 activity in NB4 and K562 cells, with an IC50s of 13.45 nM and 301 nM, respectively. RO3280 shows inhibitory activities against the growth of six leukemia cells, with IC50s of 186 nM, 175 nM, 74 nM, 797 nM, 120 nM and 162 nM for U937, HL60, NB4, K562, MV4-11 and CCRF cell lines, respectively. RO3280 also suppresses the growth of primary ALL and AML cells, with IC50s of 35.49-110.76 nM, and 52.80-147.50 nM, respectively. RO3280 (50 or 100 nM) induces apoptosis and cell cycle disorder in acute leukemia cells[1]. Ro3280 shows potent activity in H82, H69, A549 lung cancer cell lines with EC50s of 6 nM, 7 nM and 82 nM. Ro3280 also inhibits several other cancer cell lines, with low concentration[2]. RO3280 is cytotoxic to 5637 and T24 human bladder cancer cells, with IC50s of appr 100 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
RO3280 (30 mg/kg, once every 5 days, i.p.) shows significant anti-bladder cancer activities in a nude mouse model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1062243-51-9
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Appearance Solid
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Peso molecular 543.61
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Fòrmula C27H35F2N7O3
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Color Off-white to yellow
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SMILES
COC1=C(NC2=NC(N(C3CCCC3)CC(F)(F)C(N4C)=O)=C4C=N2)C=CC(C(NC5CCN(C)CC5)=O)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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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
Ro3280 purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 May 9;12(8):3911-3927. [Abstract]
Cell apoptosis assays performed by flow cytometry after treatment of Ro3280 (0, 250, 500 nM) (left panel), quantification of the cell apoptosis assay results (right panel).
Ro3280 purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 May 9;12(8):3911-3927. [Abstract]
Representative images of colony formation assay in HuCCT1 after treatment of Ro3280 (0, 15, 30 nM) (left panel), quantification of the colony formation assay results (right panel).
Ro3280 purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 May 9;12(8):3911-3927. [Abstract]
Cell cycle assays performed by flow cytometry after treatment of Ro3280 (0, 125, 500 nM) (left panel), quantification of the cell cycle assay results (right panel).
Ro3280 purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 May 9;12(8):3911-3927. [Abstract]
α-SMA mRNA levels evaluation after Ro3280 (0, 1, 2 μM) treatment in NIH/3T3 cells by qRT-PCR.
Ro3280 purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 May 9;12(8):3911-3927. [Abstract]
α-SMA protein levels evaluation after Ro3280 (0, 1, 2 μM) treatment in NIH/3T3 cells by western blotting.
Ro3280 purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 May 9;12(8):3911-3927. [Abstract]
Expression level of α-SMA after medium and Ro3280 treatment in NIH/3T3 cells by IF staining.
Ro3280 purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 May 9;12(8):3911-3927. [Abstract]
Images of livers from CCA mouse models treated with Ro3280, HA-ODA/Ro and AAHA-ODA/Ro.
Ro3280 purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 May 9;12(8):3911-3927. [Abstract]
Represntive images of liver by H&E for α-SMA treated with Ro3280, HA-ODA/Ro and AAHA-ODA/Ro.
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Cancer Lett
Inhibition of the mitotic kinase PLK1 overcomes therapeutic resistance to BET inhibitors in triple negative breast cancer. [Abstract]2020 Oct 28:491:50-59. PMID: 32735909 -
Mol Pharm
Unusually High Affinity of the PLK Inhibitors RO3280 and GSK461364 to HSA and Its Possible Pharmacokinetic Implications. [Abstract]2023 Mar 6;20(3):1631-1642. PMID: 36812406 -
J Photochem Photobiol B
Shedding light on the binding mechanism of kinase inhibitors BI-2536, Volasetib and Ro-3280 with their pharmacological target PLK1. [Abstract]2022 Jul:232:112477. PMID: 35644070
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (183.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (4.60 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 (4.60 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
In Vivo Dissolution Calculator
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.
Protocolo
Cell Assay[1]
Leukemia cells or primary leukemia cells (2 × 104) are seeded in 96-well plates overnight and incubated with DMSO, or increasing concentrations of RO3280 (0.05-120 μM) for 24 h. The same volume of DMSO added to the vehicle treated wells. Each drug concentration is replicated four times. Then, 10 μL CCK8 solution is added to each well, incubated at 37°C for 2-4 h and the optical density (OD) values are measured at 450 nm using a scanning multi-well spectrophotometer. Relative survival rate is calculated from the absorbance values compared with the control group. The proliferation of cells is calculated as a percentage of the DMSO-treated control wells with 50% inhibitory concentration (IC50) values derived after plotting proliferation values on a logarithmic curve. The IC50 of PLK1 inhibitor is calculated by Graph Prism software[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[3]
Briefly, mice (female, 4-5 weeks of age) are used in the assay. Cells (5 × 106 cells in 150 μL) are suspended in RPMI 1640 and injected subcutaneously into the flank of each BALB/c nude mouse. On day 5, tumour size is measured, the animals are randomized into two groups (n = 15 per group), and RO3280 (40 mg/kg, once every 5 days) treatment is initiated by intraperitoneal injection. The control group is treated with vehicle (1.5% DMSO in PBS). The drug (or vehicle) treatment is performed for 40 days. The length and width of the resulting tumours (in millimetres) are measured every 3 days with callipers. The tumour diameter is measured, and the volume (length × width2 × 0.52) is calculated. The mice are humanely killed on day 45, and the tumours are dissected and weighed. Western blot and immunohistochemistry assays are also performed with these sections. Then, the tumours are fixed, embedded and cut into 3‐μm‐thick sections, which are subsequently stained with haematoxylin and eosin to permit the observation of the tumour margin[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Wang NN, et al. Molecular targeting of the oncoprotein PLK1 in pediatric acute myeloid leukemia: RO3280, a novel PLK1 inhibitor, induces apoptosis in leukemia cells. Int J Mol Sci. 2015 Jan 7;16(1):1266-92. [Content Brief]
[2]. Chen S, et al. Identification of novel, potent and selective inhibitors of Polo-like kinase 1. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1247-50. [Content Brief]
[3]. Zhang Z, et al. Targeted inhibition of Polo-like kinase 1 by a novel small-molecule inhibitor induces mitotic catastrophe and apoptosis in human bladder cancer cells. J Cell Mol Med. 2017 Apr;21(4):758-767. [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 | 1.8396 mL | 9.1978 mL | 18.3955 mL | 45.9889 mL |
| 5 mM | 0.3679 mL | 1.8396 mL | 3.6791 mL | 9.1978 mL | |
| 10 mM | 0.1840 mL | 0.9198 mL | 1.8396 mL | 4.5989 mL | |
| 15 mM | 0.1226 mL | 0.6132 mL | 1.2264 mL | 3.0659 mL | |
| 20 mM | 0.0920 mL | 0.4599 mL | 0.9198 mL | 2.2994 mL | |
| 25 mM | 0.0736 mL | 0.3679 mL | 0.7358 mL | 1.8396 mL | |
| 30 mM | 0.0613 mL | 0.3066 mL | 0.6132 mL | 1.5330 mL | |
| 40 mM | 0.0460 mL | 0.2299 mL | 0.4599 mL | 1.1497 mL | |
| 50 mM | 0.0368 mL | 0.1840 mL | 0.3679 mL | 0.9198 mL | |
| 60 mM | 0.0307 mL | 0.1533 mL | 0.3066 mL | 0.7665 mL | |
| 80 mM | 0.0230 mL | 0.1150 mL | 0.2299 mL | 0.5749 mL | |
| 100 mM | 0.0184 mL | 0.0920 mL | 0.1840 mL | 0.4599 mL |
Ro3280 Related Classifications
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