JNJ-74856665
Based on 1 Customer Validation
JNJ-74856665 (DHODH-IN-16) is a potent dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 of 0.396 nM for human DHODH.
For research use only. We do not sell to patients.
- Purity: 99.74%
- CAS No.: 2511248-11-4
- Formula: C24H25FN4O3
- Molecular Weight:436.48
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
IC50: 0.396 nM (human DHODH)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
0.19 nM
Compound: 16; JNJ-74856665
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Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human MOLM-13 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo assay
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[PMID: 38889244] |
| MOLM-13 | IC50 |
0.2 nM
Compound: 22
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Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo assay
Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo assay
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[PMID: 33603957] |
JNJ-74856665 (DHODH-IN-16) (Example 22) potently inhibits the growth of MOLM-13 cells with an IC50 of 0.2 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2511248-11-4
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Appearance Solid
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Molecular Weight 436.48
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Formula C24H25FN4O3
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Color White to light yellow
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SMILES
O=C1C2=C(C(C(C)C)=CN1C3=C(C)C=CC=C3)C=C(N4N=C(CO)N(CC)C4=O)C(F)=C2
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Synonyms
DHODH-IN-16
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (229.11 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 (5.73 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.
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.
Purity & Documentation
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Data Sheet (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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 | 2.2911 mL | 11.4553 mL | 22.9106 mL | 57.2764 mL |
| 5 mM | 0.4582 mL | 2.2911 mL | 4.5821 mL | 11.4553 mL | |
| 10 mM | 0.2291 mL | 1.1455 mL | 2.2911 mL | 5.7276 mL | |
| 15 mM | 0.1527 mL | 0.7637 mL | 1.5274 mL | 3.8184 mL | |
| 20 mM | 0.1146 mL | 0.5728 mL | 1.1455 mL | 2.8638 mL | |
| 25 mM | 0.0916 mL | 0.4582 mL | 0.9164 mL | 2.2911 mL | |
| 30 mM | 0.0764 mL | 0.3818 mL | 0.7637 mL | 1.9092 mL | |
| 40 mM | 0.0573 mL | 0.2864 mL | 0.5728 mL | 1.4319 mL | |
| 50 mM | 0.0458 mL | 0.2291 mL | 0.4582 mL | 1.1455 mL | |
| 60 mM | 0.0382 mL | 0.1909 mL | 0.3818 mL | 0.9546 mL | |
| 80 mM | 0.0286 mL | 0.1432 mL | 0.2864 mL | 0.7160 mL | |
| 100 mM | 0.0229 mL | 0.1146 mL | 0.2291 mL | 0.5728 mL |