NK7-902 diTFA
Based on 1 Customer Validation
NK7-902 diTFA is a selective and orally active CRBN-dependent NEK7 molecular glue degrader with Kd values of 1.5 and 2.6 μM for hNEK7 and mNEK7. NK7-902 diTFA fully degrades NEK7 in human primary monocytes and whole blood but only partially inhibits NLRP3-dependent IL-1β production. NK7-902 diTFA shows activity in murine systems and induces a profound and long-lasting NEK7 degradation but only transiently blocks NLRP3 inflammasome activation. NK7-902 diTFA can be used for the research of inflammation, such as cryopyrin-associated periodic syndromes.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.88%
- Fòrmula: C26H28F6N4O8
- Peso molecular:638.51
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 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
Actividad biológica
Descripciòn
IC50 & Target
[1]|
NEK7 |
NLRP3 inflammasome |
IL-1β |
In Vitro
NK7-902 diTFA (0.005-10000 nM; 18 h pre-treatment) potently and selectively degrades NEK7 (DC50 = 0.2 nM) in human primary monocytes, with partial, stimulus-dependent inhibition of NLRP3 inflammasome-mediated IL-1β secretion[1].
NK7-902 diTFA (0.009-10000 nM; 18 h) potently degrades NEK7 (DC50 = 1.6 nM) in human PBMCs, with full NLRP3 inflammasome inhibition in most CAPS mutations but partial inhibition in the NEK7T348M mutation[1].
NK7-902 diTFA (0.001-10000 nM; 18 h) potently degrades NEK7 in human whole blood (DC50 = 8.7 nM) and neutrophils, with partial IL-1β inhibition in whole blood but full inhibition in isolated neutrophils[1].
NK7-902 diTFA (1-10000 nM; 18 h) potently degrades NEK7 (DC50 = 54.2 nM) in mouse primary splenocytes in a CRBN-dependent manner[1].
NK7-902 diTFA (0.1-10000 nM; 18 h) potently degrades NEK7 (DC50 = 4.1 nM) in NHP blood in vitro[1].
NK7-902 diTFA (20-411 μg/mL; 96 h) degrades NEK7 in human primary blood lymphocytes without inducing significant chromosomal damage or cell cycle delay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human primary monocytes
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Concentration:0.005, 0.026, 0.13, 0.64, 3.2, 16, 80, 40, 2000, 10000 nM
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Incubation Time:18 h pre-treatment
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Result:Induced a dose-dependently NEK7 degradation with DC50 of 0.2 nM and Dmax of >95%.
In Vivo
NK7-902 diTFA (300 mg/kg; p.o.; single dose; 16h pre-LPS challenge) induces robust NEK7 degradation and significant inhibition of NLRP3 inflammasome-mediated IL-1β release in a mouse CAPS model[1].
NK7-902 diTFA (0.2-2 mg/kg; p.o.; single dose) induces profound, long-lasting NEK7 degradation but only transient IL-1β inhibition in non-human primates[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Acute peritonitis C57BL/6JRj mice (female, 7-8 weeks old)[1]
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Dosage:30 mg/kg; 100 mg/kg; 300 mg/kg
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Administration:P.o.; single dose; 6h pre-LPS challenge; 16h pre-LPS challenge
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Result:Induced dose-dependent NEK7 degradation in mouse spleen, with maximum degradation observed at the 300 mg/kg dose at the 8h + 15min time point.
Showed slight recovery of NEK7 protein levels at the 18h + 15min time point.
Accompanied dose-dependent inhibition of IL-1β release in peritoneal lavage fluid.
Chemical Information
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Appearance Solid
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Peso molecular 638.51
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Fòrmula C26H28F6N4O8
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Color Light yellow to yellow
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SMILES
CCN[C@@H]1CC[C@@H]2N(C3=CC=C(C(N(C4CCC(NC4=O)=O)C5=O)=O)C5=C3)[C@H]1CC2.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O
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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 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (156.61 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)
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 (3.92 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 (3.92 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.
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (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, 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 |
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| DMSO | 1 mM | 1.5661 mL | 7.8307 mL | 15.6615 mL | 39.1537 mL |
| 5 mM | 0.3132 mL | 1.5661 mL | 3.1323 mL | 7.8307 mL | |
| 10 mM | 0.1566 mL | 0.7831 mL | 1.5661 mL | 3.9154 mL | |
| 15 mM | 0.1044 mL | 0.5220 mL | 1.0441 mL | 2.6102 mL | |
| 20 mM | 0.0783 mL | 0.3915 mL | 0.7831 mL | 1.9577 mL | |
| 25 mM | 0.0626 mL | 0.3132 mL | 0.6265 mL | 1.5661 mL | |
| 30 mM | 0.0522 mL | 0.2610 mL | 0.5220 mL | 1.3051 mL | |
| 40 mM | 0.0392 mL | 0.1958 mL | 0.3915 mL | 0.9788 mL | |
| 50 mM | 0.0313 mL | 0.1566 mL | 0.3132 mL | 0.7831 mL | |
| 60 mM | 0.0261 mL | 0.1305 mL | 0.2610 mL | 0.6526 mL | |
| 80 mM | 0.0196 mL | 0.0979 mL | 0.1958 mL | 0.4894 mL | |
| 100 mM | 0.0157 mL | 0.0783 mL | 0.1566 mL | 0.3915 mL |
NK7-902 diTFA Related Classifications
HY-173154B Related Classifications
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