KME-2780
Based on 1 Customer Validation
KME-2780 is the orally active inhibitor for IRAK1 and IRAK4 with IC50s of 19 nM and 0.5 nM. KME-2780 can be used for research of dysregulation of innate immune signaling and hematologic malignancies.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.94%
- CAS No.: 2968466-26-2
- Formule: C20H23N5
- Masse moléculaire:333.43
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Stockage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Immunology/Inflammation Compound Library
HY-L007
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Kinase Inhibitor Library
HY-L009
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Anti-Cancer Compound Library
HY-L025
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Clinical Compound Library
HY-L026
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Drug Repurposing Compound Library
HY-L035
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Orally Active Compound Library
HY-L061
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Cell Death Library
HY-L162
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Serine/Threonine Kinase Inhibitor Library
HY-L164
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Drug Repurposing Compound Library Plus
HY-L035P
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Clinical Compound Library Plus
HY-L026P
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Bioactive Compound Library
HY-L001
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Protein Kinase Compound Library
HY-L196
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
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Anti-Rheumatic Arthritis Compound Library
HY-L210
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Posttranslational Modification Library
HY-L226
Activité biologique
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IRAK4 0.5 nM (IC50) |
IRAK1 19 nM (IC50) |
KME-2780 (0-1 μM, 21 days) induces apoptosis in cells MDSL, THP1, OCIAML3, AML1714 and AML1294, inhibits the colony formation of cells MDSL, THP1, OCIAML3, AML1714, AML1294, AML08 and MDS. KME-2780 promotes the differentiation of leukemic stem/progenitor cell (LSPC), upregulates the expression of CD38, and induces heterogeneous morphological changes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDSL, THP1, OCIAML3, AML1714 and AML1294
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Concentration:500 nM
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Incubation Time:48 h
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Result:Induced apoptosis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse xenograft models[1]
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Dosage:100 mg/kg/day
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Administration:po for 48 days
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Result:Reduced leukemia cell colonization in peripheral blood, improved the mice survival.
Chemical Information
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CAS No. 2968466-26-2
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Appearance Solid
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Masse moléculaire 333.43
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Formule C20H23N5
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Color White to yellow
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SMILES
CC1(CC1)C2=CN3C(C4=CC=CC(N[C@H]5CCNC5)=N4)=CN=C3C=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
DMSO : 100 mg/mL (299.91 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 (protect from light). 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 (protect from light). 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 (7.50 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Pureté et documentation
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Fiche technique (275 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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Instruction de manipulation (2659 KB)
Références
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 (protect from light). 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 | 2.9991 mL | 14.9957 mL | 29.9913 mL | 74.9783 mL |
| 5 mM | 0.5998 mL | 2.9991 mL | 5.9983 mL | 14.9957 mL | |
| 10 mM | 0.2999 mL | 1.4996 mL | 2.9991 mL | 7.4978 mL | |
| 15 mM | 0.1999 mL | 0.9997 mL | 1.9994 mL | 4.9986 mL | |
| 20 mM | 0.1500 mL | 0.7498 mL | 1.4996 mL | 3.7489 mL | |
| 25 mM | 0.1200 mL | 0.5998 mL | 1.1997 mL | 2.9991 mL | |
| 30 mM | 0.1000 mL | 0.4999 mL | 0.9997 mL | 2.4993 mL | |
| 40 mM | 0.0750 mL | 0.3749 mL | 0.7498 mL | 1.8745 mL | |
| 50 mM | 0.0600 mL | 0.2999 mL | 0.5998 mL | 1.4996 mL | |
| 60 mM | 0.0500 mL | 0.2499 mL | 0.4999 mL | 1.2496 mL | |
| 80 mM | 0.0375 mL | 0.1874 mL | 0.3749 mL | 0.9372 mL | |
| 100 mM | 0.0300 mL | 0.1500 mL | 0.2999 mL | 0.7498 mL |
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