MIR002
Based on 1 Customer Validation
MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.0%
- No. CAS: 2217671-64-0
- Fòrmula: C27H29NO5
- Peso molecular:447.52
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
- Pureza y Documentación
- Referencias
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Help & FAQs
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Apoptosis Compound Library
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Cell Cycle/DNA Damage Compound Library
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Epigenetics Compound Library
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Histone Modification Research Compound Library
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Anti-Cancer Compound Library
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Anti-Aging Compound Library
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Reprogramming Compound Library
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Oxygen Sensing Compound Library
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Orally Active Compound Library
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Anti-Breast Cancer Compound Library
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Anti-Pancreatic Cancer Compound Library
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Anti-Blood Cancer Compound Library
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Anti-Liver Cancer Compound Library
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Osteogenesis Compound Library
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Highly Selective Inhibitors Library
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Highly Selective Activators Library
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Cell Death Library
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Anti-Hematopathy Compound Library
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Multi-Target Compound Library
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Bioactive Compound Library Max
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Anti-Brain Cancer Compound Library
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
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Cell Proliferation Compound Library
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High-Efficiency Gene Editing Compound Library
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Lactylation Compound Library
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Actividad biológica
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HDAC11 6.09 μM (IC50) |
DNA Polymerase |
POLA1 |
MIR002 (24 h) shows antiproliferative activity at nanomolar concentrations (IC50s of 0.25, 2.8, 0.6, 0.41 μM in NCI-H460, H460-R9A, A2780, A2780-DX; IC50s of 0.9, 1.2, 0.22, 0.71, 2.1, 0.52, 0.038, 0.18, 0.42, 1.9, 0.64, 1.1 μM in MM432, MM473, MM487, RAMOS, L-428, U-293, Z-138, NB4, THP-1, MDA-MB231, MDA-MB436, U87MG cells, respectively)[1].
MIR002 (0.0001,0.01, 1, 10 μM) shows inhibitory activity on HDAC11 with an IC50 of 6.09 μM[1].
MIR002 (0.1, 0.25, 0.4 μM, 24 h) shows a dose-dependent p53 acetylation and p21 induction as well as H2AX Phosphorylation[1]. MIR002 (72 h) leads to cell cycle arrest at the G1-S phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM432, MM473, MM487, RAMOS, L-428, U-293, Z-138, NB4, THP-1, MDA-MB231, MDA-MB436, U87MG cells
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Concentration:10 scalar concentrations
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Incubation Time:24 h
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Result:Showed antiproliferative activity at nanomolar concentrations (IC50s of 0.9, 1.2, 0.22, 0.71, 2.1, 0.52, 0.038, 0.18, 0.42, 1.9, 0.64, 1.1 µM in MM432, MM473, MM487, RAMOS, L-428, U-293, Z-138, NB4, THP-1, MDA-MB231, MDA-MB436, U87MG cells, respectively)
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Cell Line:NCI-H460, MM473, MM487, A2780 cells
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Concentration:0.1, 0.25, 0.4 µM
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Incubation Time:24 h
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Result:Showed antiproliferative activity at nanomolar concentrations (IC50s of 0.9, 1.2, Showed a dosedependent p53 acetylation and p21 induction as well as H2AX Phosphorylation.
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Cell Line:NCI-H460, A2780, MM473, H460-R9A cells
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Concentration:0.25 µM for NCI-H460, 0.6 µM for A2780, 1.2 µM for MM473, 2.8 µM for H460-R9A
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Incubation Time:72 h
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Result:Cells were arrested at the G1-S phase.
MIR002 (50 mg/kg; p.o.; twice a day for 5 days a week, 6 weeks) shows an additive antitumor effect with complete disappearance of tumor masses in two animals at the end of the treatment when combination with cisplatin[1].
MIR002 ( 50 mg/kg, twice a day for 5 days) induces a significant increase of a interferon at its pharmacological active dose (50 mg/kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Model: 4-6 weeks old female CD-1 nude mice (NSCLC NCI-H460 model)
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Dosage:50 mg/kg
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Administration:p.o.; twice a day for 5 days a week, 3 weeks
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Result:Showed a good tolerability and antitumor activity (TGI=61%).
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Animal Model:4-6 weeks old female CD-1 nude mice ( MM473-luc and MM487-Luc)[1]
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Dosage:50 mg/kg combibnated with cisplatin (i.p.; 5 mg/kg; twice a day for 7 days a week, 6 weeks)
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Administration:p.o.; twice a day for 5 days a week, 6 weeks
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Result:Showed an additive antitumor effect with complete disappearance of tumor masses in two animals at the end of the treatment when combination with cisplatin.
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Animal Model:4-6 weeks old female CD-1 nude mice (Melanoma B16 model)[1]
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Dosage:50 mg/kg
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Administration:p.o.; twice a day for 5 days
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Result:Induced a significant increase of α interferon at its pharmacological active dose (50 mg/kg).
Chemical Information
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No. CAS 2217671-64-0
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Appearance Solid
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Peso molecular 447.52
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Fòrmula C27H29NO5
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Color White to off-white
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SMILES
ONC(COC1=C(C=C(C2=CC=C(C=C2)/C=C/C(O)=O)C=C1)C34CC5CC(CC(C5)C4)C3)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (223.45 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.59 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.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2345 mL | 11.1727 mL | 22.3454 mL | 55.8634 mL |
| 5 mM | 0.4469 mL | 2.2345 mL | 4.4691 mL | 11.1727 mL | |
| 10 mM | 0.2235 mL | 1.1173 mL | 2.2345 mL | 5.5863 mL | |
| 15 mM | 0.1490 mL | 0.7448 mL | 1.4897 mL | 3.7242 mL | |
| 20 mM | 0.1117 mL | 0.5586 mL | 1.1173 mL | 2.7932 mL | |
| 25 mM | 0.0894 mL | 0.4469 mL | 0.8938 mL | 2.2345 mL | |
| 30 mM | 0.0745 mL | 0.3724 mL | 0.7448 mL | 1.8621 mL | |
| 40 mM | 0.0559 mL | 0.2793 mL | 0.5586 mL | 1.3966 mL | |
| 50 mM | 0.0447 mL | 0.2235 mL | 0.4469 mL | 1.1173 mL | |
| 60 mM | 0.0372 mL | 0.1862 mL | 0.3724 mL | 0.9311 mL | |
| 80 mM | 0.0279 mL | 0.1397 mL | 0.2793 mL | 0.6983 mL | |
| 100 mM | 0.0223 mL | 0.1117 mL | 0.2235 mL | 0.5586 mL |
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