KTX-582
Based on 1 Customer Validation
KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.65%
- No. CAS: 2573298-13-0
- Fòrmula: C45H51F3N8O7
- Peso molecular:872.93
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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
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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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Actividad biológica
DC50: 4 nM (IRAK4), 5 nM (Ikaros)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| OCI-Ly10 | IC50 |
14 nM
Compound: 16
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Antiproliferative activity against human OCI-Ly10 cells measured after 4 days by CellTiter-Glo Luminescent Cell Viability Assay
Antiproliferative activity against human OCI-Ly10 cells measured after 4 days by CellTiter-Glo Luminescent Cell Viability Assay
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[PMID: 38920289] |
KTX-582 (compound I-41) degrades IRAK4 in whole blood monocyte and lymphocyte with IC50s of <0.05 μM[4].
KTX-582 inhibits IRAK4 in human whole blood LPS TNFα with an IC50 of 0.05~1 μM[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2573298-13-0
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Appearance Solid
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Peso molecular 872.93
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Fòrmula C45H51F3N8O7
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Color Light yellow to yellow
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SMILES
O=C(C1=NC(C(F)(F)F)=CC=C1)NC2=CC3=CN([C@H]4CC[C@H](CN(CCCO[C@H]5C[C@H](NC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)C5)C)CC4)N=C3C=C2C(C)(O)C
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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
DMSO : 100 mg/mL (114.56 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.86 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 (2.86 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 (272 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1456 mL | 5.7278 mL | 11.4557 mL | 28.6392 mL |
| 5 mM | 0.2291 mL | 1.1456 mL | 2.2911 mL | 5.7278 mL | |
| 10 mM | 0.1146 mL | 0.5728 mL | 1.1456 mL | 2.8639 mL | |
| 15 mM | 0.0764 mL | 0.3819 mL | 0.7637 mL | 1.9093 mL | |
| 20 mM | 0.0573 mL | 0.2864 mL | 0.5728 mL | 1.4320 mL | |
| 25 mM | 0.0458 mL | 0.2291 mL | 0.4582 mL | 1.1456 mL | |
| 30 mM | 0.0382 mL | 0.1909 mL | 0.3819 mL | 0.9546 mL | |
| 40 mM | 0.0286 mL | 0.1432 mL | 0.2864 mL | 0.7160 mL | |
| 50 mM | 0.0229 mL | 0.1146 mL | 0.2291 mL | 0.5728 mL | |
| 60 mM | 0.0191 mL | 0.0955 mL | 0.1909 mL | 0.4773 mL | |
| 80 mM | 0.0143 mL | 0.0716 mL | 0.1432 mL | 0.3580 mL | |
| 100 mM | 0.0115 mL | 0.0573 mL | 0.1146 mL | 0.2864 mL |
KTX-582 Related Classifications
HY-148274 Related Classifications
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