BLU2864
Based on 2 publication(s) in Google Scholar
BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research.
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- Pureza: 99.50%
- No. CAS: 2810747-89-6
- Fòrmula: C24H19F3N4O2
- Peso molecular:452.43
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Publications Citing Use of MedChemExpress (MCE) BLU2864
More
Actividad biológica
IC50: 0.3 nM (PRKACA)[2]
BLU2864 (40 nM and 200 nM; 5 d) inhibits forskolin (HY-15371)-induced in vitro cystogenesis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:mIMCD3 cells
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Concentration:40 nM and 200 nM
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Incubation Time:5 days
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Result:Inhibited forskolin induced in vitro cystogenesis of mIMCD3 cells cultured in Matrigel by 72% and 100% at 40 and 200 nM concentrations, respectively, relative to control.
BLU2864 (oral gavage; 30 mg/kg; once daily; 5 d) inhibits PKA activity and ameliorates PKD in Pkd1RC/RC mice[1].
BLU2864 (oral gavage; 30 mg/kg and 75 mg/kg; once daily; 34 d) reduces FLC tumor growth in vivo[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pkd1RC/RC mice[1]
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Dosage:45 mg/kg
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Administration:Oral gavage; 45 mg/kg; once daily; 5 days
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Result:Suppressed kidney basal and total PKA activities by 74% and 87% at 3 hours and by 46% and 56% at 15 hours, respectively, in the BLU2864-treated mice compared with controls.
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Animal Model:Pkd1RC/RC mice[1]
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Dosage:30 mg/kg
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Administration:Oral gavage; 30 mg/kg; once daily; 5 days
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Result:Showed higher urine outputs at 15 weeks in the BLU2864-treated mice than in the controls. Showed lower kidney weights, kidney volumes as percent of body weights, and cyst indices. Showed renal basal and total PKA activities by 69% and 84% lower in the BLU2864-treated mice compared with controls.
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Animal Model:Mice harboring FLC PDX tumors[2]
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Dosage:30 mg/kg and 75 mg/kg
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Administration:Oral gavage; 30 mg/kg and 75 mg/kg; once daily; 34 days
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Result:Inhibited tumor growth by 48.5% (P=0.003) and by 45.3% (P=0.0005), respectively, at day 34.
Chemical Information
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No. CAS 2810747-89-6
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Appearance Solid
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Peso molecular 452.43
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Fòrmula C24H19F3N4O2
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Color Off-white to light yellow
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SMILES
FC1=CC(C(F)F)=CC2=C1[C@H]([C@@H](O)C2)NC(C(C=C3)=CN=C3C4=C(C(C)=CN5)C5=NC=C4)=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 (2)
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Journal Impact Factor
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Most Recent
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Bioorg Med Chem
Identification of a novel Aurora B inhibitor using the AI-driven drug screening and docking-based traditional screening. [Abstract]2025 Sep 27:131:118423. PMID: 41033076 -
bioRxiv
2026 Mar 31:2026.03.29.715116. PMID: 41959225
Solvente y solubilidad
DMSO : 100 mg/mL (221.03 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 (5.53 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.53 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 (279 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 | 2.2103 mL | 11.0514 mL | 22.1029 mL | 55.2572 mL |
| 5 mM | 0.4421 mL | 2.2103 mL | 4.4206 mL | 11.0514 mL | |
| 10 mM | 0.2210 mL | 1.1051 mL | 2.2103 mL | 5.5257 mL | |
| 15 mM | 0.1474 mL | 0.7368 mL | 1.4735 mL | 3.6838 mL | |
| 20 mM | 0.1105 mL | 0.5526 mL | 1.1051 mL | 2.7629 mL | |
| 25 mM | 0.0884 mL | 0.4421 mL | 0.8841 mL | 2.2103 mL | |
| 30 mM | 0.0737 mL | 0.3684 mL | 0.7368 mL | 1.8419 mL | |
| 40 mM | 0.0553 mL | 0.2763 mL | 0.5526 mL | 1.3814 mL | |
| 50 mM | 0.0442 mL | 0.2210 mL | 0.4421 mL | 1.1051 mL | |
| 60 mM | 0.0368 mL | 0.1842 mL | 0.3684 mL | 0.9210 mL | |
| 80 mM | 0.0276 mL | 0.1381 mL | 0.2763 mL | 0.6907 mL | |
| 100 mM | 0.0221 mL | 0.1105 mL | 0.2210 mL | 0.5526 mL |
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