Pelabresib
Based on 1 Customer Validation
Pelabresib (CPI-0610) is a potent, selective, orally active and cell-active BET inhibitor. Pelabresib inhibits BRD4-BD1 with an IC50 of 39 nM, and with an EC50 value of 0.18 μM for MYC.
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- Pureza: 99.95%
- No. CAS: 1380087-89-7
- Fòrmula: C20H16ClN3O2
- Peso molecular:365.81
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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
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Actividad biológica
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BRD4-BD1 39 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | IC50 |
120 nM
Compound: CPI-0610
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In vivo inhibition of BRD4 in human MV4-11 cells xenografted in mouse tumor model
In vivo inhibition of BRD4 in human MV4-11 cells xenografted in mouse tumor model
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[PMID: 33460833] |
Pelabresib (0-1500 nM; 72 hours; Multiple myeloma cell lines and primary MM cells) treatment reduces the viability of MM cells in a dose-dependent manner[2].
Pelabresib (800 nM; 72 hours; INA6 and MM.1S cells) treatment leads to G1 cell cycle arrest[2].
Pelabresib (800 nM; 72 hours; INA6 and MM.1S cells) treatment significantly increases apoptosis in MM cells after 72 hours[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Multiple myeloma (MM) cell lines and primary MM cells
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Concentration:0 nM, 200 nM, 400 nM, 600 nM , 800 nM, 1000 nM, 1200 nM, or 1500 nM
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Incubation Time:72 huors
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Result:Decreased viability of MM cells in a dose-dependent manner.
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Cell Line:INA6 and MM.1S cells
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Concentration:800 nM
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Incubation Time:72 hours
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Result:Indeced G1 cell cycle arrest.
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Cell Line:INA6 and MM.1S cells
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Concentration:800 nM
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Incubation Time:72 hours
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Result:MM cells apoptosis was increased after 72 hours.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV-4-11 mouse xenograft model[1]
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Dosage:30 mg/kg once daily, 30 mg/kg twice daily, or 60 mg/kg once daily
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Administration:Oral administration; for 28 days
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Result:Suppressed of tumor growth, without any significant body weight loss in the animals.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1380087-89-7
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Appearance Solid
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Peso molecular 365.81
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Fòrmula C20H16ClN3O2
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Color White to off-white
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SMILES
O=C(N)C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=CC=CC=C3C4=C1ON=C4C
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Synonyms
CPI-0610
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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 (273.37 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 (5.69 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 (5.69 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.
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Albrecht BK, et al. Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials. J Med Chem. 2016 Feb 25;59(4):1330-9. [Content Brief]
[2]. Siu KT, et al. Preclinical activity of CPI-0610, a novel small-molecule bromodomain and extra-terminal protein inhibitor in the therapy of multiple myeloma. Leukemia. 2017 Aug;31(8):1760-1769. [Content Brief]
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 | 2.7337 mL | 13.6683 mL | 27.3366 mL | 68.3415 mL |
| 5 mM | 0.5467 mL | 2.7337 mL | 5.4673 mL | 13.6683 mL | |
| 10 mM | 0.2734 mL | 1.3668 mL | 2.7337 mL | 6.8341 mL | |
| 15 mM | 0.1822 mL | 0.9112 mL | 1.8224 mL | 4.5561 mL | |
| 20 mM | 0.1367 mL | 0.6834 mL | 1.3668 mL | 3.4171 mL | |
| 25 mM | 0.1093 mL | 0.5467 mL | 1.0935 mL | 2.7337 mL | |
| 30 mM | 0.0911 mL | 0.4556 mL | 0.9112 mL | 2.2780 mL | |
| 40 mM | 0.0683 mL | 0.3417 mL | 0.6834 mL | 1.7085 mL | |
| 50 mM | 0.0547 mL | 0.2734 mL | 0.5467 mL | 1.3668 mL | |
| 60 mM | 0.0456 mL | 0.2278 mL | 0.4556 mL | 1.1390 mL | |
| 80 mM | 0.0342 mL | 0.1709 mL | 0.3417 mL | 0.8543 mL | |
| 100 mM | 0.0273 mL | 0.1367 mL | 0.2734 mL | 0.6834 mL |
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