BMS-P5 free base
Based on 1 Customer Validation
BMS-P5 free base is a selective and orally active peptidylarginine deiminase 4 (PAD4) inhibitor with an IC50 of 98 nM. BMS-P5 free base shows selective for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 free base blocks multiple myeloma (MM)-induced neutrophil extracellular trap (NET) formation and delays progression of MM in a syngeneic mouse model.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 1550371-22-6
- Formula: C27H32N6O2
- Molecular Weight:472.58
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
BMS-P5 blocks calcium ionophore-induced citrullination of histone H3[1].
BMS-P5 is also able to inhibit formation of NETs induced by primary MM cells isolated from the BM of patients with MM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Neutrophils.
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Concentration:10 µM and 100 µM.
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Incubation Time:30 min followed by addition of DP42 or 5TGM1 CM.
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Result:Prevented MM-induced NET formation.
BMS-P5 (50 mg/kg, oral gavage) may attenuate the presence of pro-tumorigenic proteins in the tumor microenvironment, and thus delay tumor progression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Syngeneic mouse model of MM[1].
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Dosage:50 mg/kg.
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Administration:Oral gavage, twice a day beginning on day 3 after tumor cell injection.
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Result:Significantly delayed development of symptoms and significantly prolonged survival of MM-bearing mice.
Chemical Information
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CAS No. 1550371-22-6
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Appearance Solid
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Molecular Weight 472.58
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Formula C27H32N6O2
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Color White to off-white
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SMILES
O=C(N1[C@@H](C)CC[C@@H](N)C1)C2=CC(OC)=C3C(N=C(C4=CC5=CC=CN=C5N4CC6CC6)N3C)=C2
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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 : 250 mg/mL (529.01 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 (4.40 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.40 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 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.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 | 2.1160 mL | 10.5802 mL | 21.1604 mL | 52.9011 mL |
| 5 mM | 0.4232 mL | 2.1160 mL | 4.2321 mL | 10.5802 mL | |
| 10 mM | 0.2116 mL | 1.0580 mL | 2.1160 mL | 5.2901 mL | |
| 15 mM | 0.1411 mL | 0.7053 mL | 1.4107 mL | 3.5267 mL | |
| 20 mM | 0.1058 mL | 0.5290 mL | 1.0580 mL | 2.6451 mL | |
| 25 mM | 0.0846 mL | 0.4232 mL | 0.8464 mL | 2.1160 mL | |
| 30 mM | 0.0705 mL | 0.3527 mL | 0.7053 mL | 1.7634 mL | |
| 40 mM | 0.0529 mL | 0.2645 mL | 0.5290 mL | 1.3225 mL | |
| 50 mM | 0.0423 mL | 0.2116 mL | 0.4232 mL | 1.0580 mL | |
| 60 mM | 0.0353 mL | 0.1763 mL | 0.3527 mL | 0.8817 mL | |
| 80 mM | 0.0265 mL | 0.1323 mL | 0.2645 mL | 0.6613 mL | |
| 100 mM | 0.0212 mL | 0.1058 mL | 0.2116 mL | 0.5290 mL |