OT-82
Based on 2 publication(s) in Google Scholar
OT-82 is a potent, selective and orally active inhibitor of NAMPT. OT-82 is selectively toxic to cells of hematopoietic origin and?induces cell death in a NAD+ dependent manner. OT-82 is a promising antineoplastic agent for the study of hematological malignancies.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.95%
- No. CAS: 1800487-55-1
- Fòrmula: C26H21FN4O
- Peso molecular:424.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) OT-82
MoreVer todos los productos específicos de isoformas Caspase
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Actividad biológica
IC50: Nampt[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PANC-1 | EC50 |
3.5 nM
Compound: OT-82
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Cytotoxicity against human PANC-1 cells assessed as reduction in cell viability measured after 72 hrs by by resazurin staining based fluorescent plate reader
Cytotoxicity against human PANC-1 cells assessed as reduction in cell viability measured after 72 hrs by by resazurin staining based fluorescent plate reader
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[PMID: 35724566] |
OT-82 (0.0001-10 μM; 72 hours) demonstrates tissue-selective (HP vs non-HP) cytotoxicity. It is against HP cell lines MV4–11, U937, RS4;11, HEL92.1.7 and PER485 cell growth with IC50 values of 2.11 nM, 2.70 nM, 1.05 nM and 1.36 nM, respectively. It also against nonHP cell lines MCF-7, U87, HT29, and H1299 cell growth with IC50 values of 37.92 nM, 29.52 nM, 15.67 nM and 7.95 nM , respectively[1]. OT-82 demonstrates cancer-selective (tumor vs normal) cytotoxicity. It more sensitive to BMMNC from leukemia patients, the IC50 values are 31 nM and 7.10 nM for AML and ALL donors, respectively. The IC50 value is 62.69 nM for BMMNC from healthy donors[1]. OT-82 (0.001-10 μM; 48 hours) inhibits recombinant NAMPT activity and causes dose-dependent reductions in cellular NAD and ATP concentrations in MV4–11 cells[1].OT-82 (0.01-100 nM; 48 hours) results in activation of caspase-3, an increase in the proportion of cells with sub-G1 DNA content, and depolarization of the mitochondrial membrane in MV4–11 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HP cell lines (MV4–11, U937, RS4;11, HEL92.1.7, PER485)Non-HP cell lines (MCF-7, U87, HT29, H1299)
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Concentration:0.0001 μM-10 μM
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Incubation Time:72 hours
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Result:Was against human cell lines derived from hematological malignancies (HP) with IC50 values ranging from 1.10 nM to 5.86 nM, and was against non-HP cancers with IC50 ranging from 1.10 nM to 37.92 nM[1].
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Cell Line:MV4–11 cells
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Concentration:0.01-100 nM
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Incubation Time:48 hours
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Result:Exhibited hallmarks of apoptotic cell death
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SC xenograft model of Burkitt's lymphoma in SCID mice[1]
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Dosage:20 or 40 mg/kg
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Administration:oral gavage; 3 weeks
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Result:Potently inhibited tumor growth of multiple myeloma mouse model.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1800487-55-1
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Appearance Solid
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Peso molecular 424.47
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Fòrmula C26H21FN4O
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Color White to light yellow
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SMILES
O=C(NCCCC1=CNN=C1)C2=CC=C(C3=CC=NC=C3)C(C#CC4=CC=C(F)C=C4)=C2
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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 (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
G-CSF/NAMPT signaling drives neutrophil dysfunction and enhances bacterial infection susceptibility in cancer patients. [Abstract]2025 Dec 12;16(1):11137. PMID: 41387444 -
Solvente y solubilidad
DMSO : 100 mg/mL (235.59 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)
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: ≥ 2.08 mg/mL (4.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (276 KB)
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SDS (251 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, 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 | 2.3559 mL | 11.7794 mL | 23.5588 mL | 58.8970 mL |
| 5 mM | 0.4712 mL | 2.3559 mL | 4.7118 mL | 11.7794 mL | |
| 10 mM | 0.2356 mL | 1.1779 mL | 2.3559 mL | 5.8897 mL | |
| 15 mM | 0.1571 mL | 0.7853 mL | 1.5706 mL | 3.9265 mL | |
| 20 mM | 0.1178 mL | 0.5890 mL | 1.1779 mL | 2.9448 mL | |
| 25 mM | 0.0942 mL | 0.4712 mL | 0.9424 mL | 2.3559 mL | |
| 30 mM | 0.0785 mL | 0.3926 mL | 0.7853 mL | 1.9632 mL | |
| 40 mM | 0.0589 mL | 0.2945 mL | 0.5890 mL | 1.4724 mL | |
| 50 mM | 0.0471 mL | 0.2356 mL | 0.4712 mL | 1.1779 mL | |
| 60 mM | 0.0393 mL | 0.1963 mL | 0.3926 mL | 0.9816 mL | |
| 80 mM | 0.0294 mL | 0.1472 mL | 0.2945 mL | 0.7362 mL | |
| 100 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.5890 mL |
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