BMS-986242
Based on 1 publication(s) in Google Scholar
BMS-986242 is an orally active, potent and selective indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor. BMS-986242 can be used for the research of cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.85%
- No. CAS: 1923844-48-7
- Fòrmula: C24H24ClFN2O
- Peso molecular:410.91
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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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Publications Citing Use of MedChemExpress (MCE) BMS-986242
More
Actividad biológica
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IDO1 |
BMS-986242 is more prone to oxidative metabolism and less susceptible to glucuronidation. BMS-986242 shows IC50>25 μM for all targets except nAChR a1 (IC50=12.3 μM) and nAChR a7 (IC50>6 μM with ～20 % max inhibition)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:nu/nu Mouse[1]
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Dosage:3~30 mg/kg
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Administration:P.o.
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Result:Exhibited dose-proportional exposure and a statistically significant reduction in kynurenine concentration in the tumor at all three doses.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1923844-48-7
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Appearance Solid
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Peso molecular 410.91
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Fòrmula C24H24ClFN2O
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Color White to off-white
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SMILES
FC1=CC2=C(C=C1)N=CC=C2[C@H]3CC[C@@](CC3)([H])[C@@H](C)NC(C4=CC=C(C=C4)Cl)=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
Publications (1)
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Journal Impact Factor
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Most Recent
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Toxicol Appl Pharmacol
Indoleamine 2,3-dioxygenase 1 regulates breast cancer tamoxifen resistance through interleukin-6/signal transducer and activator of transcription. [Abstract]2022 Apr 1:440:115921. PMID: 35157906
Solvente y solubilidad
DMSO : 250 mg/mL (608.41 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: ≥ 2.08 mg/mL (5.06 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.
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 (273 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 | 2.4336 mL | 12.1681 mL | 24.3362 mL | 60.8406 mL |
| 5 mM | 0.4867 mL | 2.4336 mL | 4.8672 mL | 12.1681 mL | |
| 10 mM | 0.2434 mL | 1.2168 mL | 2.4336 mL | 6.0841 mL | |
| 15 mM | 0.1622 mL | 0.8112 mL | 1.6224 mL | 4.0560 mL | |
| 20 mM | 0.1217 mL | 0.6084 mL | 1.2168 mL | 3.0420 mL | |
| 25 mM | 0.0973 mL | 0.4867 mL | 0.9734 mL | 2.4336 mL | |
| 30 mM | 0.0811 mL | 0.4056 mL | 0.8112 mL | 2.0280 mL | |
| 40 mM | 0.0608 mL | 0.3042 mL | 0.6084 mL | 1.5210 mL | |
| 50 mM | 0.0487 mL | 0.2434 mL | 0.4867 mL | 1.2168 mL | |
| 60 mM | 0.0406 mL | 0.2028 mL | 0.4056 mL | 1.0140 mL | |
| 80 mM | 0.0304 mL | 0.1521 mL | 0.3042 mL | 0.7605 mL | |
| 100 mM | 0.0243 mL | 0.1217 mL | 0.2434 mL | 0.6084 mL |
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