Ibrutinib-MPEA
Based on 1 Customer Validation
Ibrutinib-MPEA is an orally active, blood-brain barrier permeable inhibitor of BTK and STAT5. As a derivative of Ibrutinib (HY-10997) conjugated with a PROTAC linker, Ibrutinib-MPEA allows the synthesis of a series of PROTAC molecules. Ibrutinib-MPEA significantly reduces the proliferation of neoplastic mast cells and primary mastocytoma cells by inducing apoptosis and inhibiting IgE-dependent histamine release. Ibrutinib-MPEA is applicable to the research of canine mast cell tumors, cerebral ischemia/reperfusion injury in diabetic mice, and neuroinflammation-related diseases.
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- Pureté : 99.71%
- CAS No.: 1710768-30-1
- Formule: C32H39N9O2
- Masse moléculaire:581.71
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
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STAT5 |
In Vitro
Ibrutinib-MPEA serves as a conjugate of Btk ligand and linker for the synthesis of a series of PROTAC molecules, such as P13I. When applied to human Burkitt's lymphoma RAMOS cells, P13I degrades 73% and 89% of Btk at concentrations of 10 and 100 nM, respectively[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1710768-30-1
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Appearance Solid
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Masse moléculaire 581.71
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Formule C32H39N9O2
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Color White to yellow
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SMILES
NCCN1CCN(C/C=C/C(N2C[C@H](N3N=C(C4=CC=C(OC5=CC=CC=C5)C=C4)C6=C(N)N=CN=C63)CCC2)=O)CC1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 33.33 mg/mL (57.30 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)
In Vivo:
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: ≥ 3.33 mg/mL (5.72 mM); Clear solution
This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 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 (4.30 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 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.
In Vivo Dissolution Calculator
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.
Pureté et documentation
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Fiche technique (273 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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Instruction de manipulation (2659 KB)
Références
[1]. Gamperl S, et al. Effects of ibrutinib on proliferation and histamine release in canine neoplastic mast cells. Vet Comp Oncol. 2019;17(4):553-561. [Content Brief]
[2]. Jin L, et al. Ibrutinib ameliorates cerebral ischemia/reperfusion injury through autophagy activation and PI3K/Akt/mTOR signaling pathway in diabetic mice. Bioengineered. 2021;12(1):7432-7445. [Content Brief]
[3]. Nam HY, et al. Ibrutinib suppresses LPS-induced neuroinflammatory responses in BV2 microglial cells and wild-type mice. J Neuroinflammation. 2018;15(1):271. Published 2018 Sep 19. [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 |
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| DMSO | 1 mM | 1.7191 mL | 8.5953 mL | 17.1907 mL | 42.9767 mL |
| 5 mM | 0.3438 mL | 1.7191 mL | 3.4381 mL | 8.5953 mL | |
| 10 mM | 0.1719 mL | 0.8595 mL | 1.7191 mL | 4.2977 mL | |
| 15 mM | 0.1146 mL | 0.5730 mL | 1.1460 mL | 2.8651 mL | |
| 20 mM | 0.0860 mL | 0.4298 mL | 0.8595 mL | 2.1488 mL | |
| 25 mM | 0.0688 mL | 0.3438 mL | 0.6876 mL | 1.7191 mL | |
| 30 mM | 0.0573 mL | 0.2865 mL | 0.5730 mL | 1.4326 mL | |
| 40 mM | 0.0430 mL | 0.2149 mL | 0.4298 mL | 1.0744 mL | |
| 50 mM | 0.0344 mL | 0.1719 mL | 0.3438 mL | 0.8595 mL |
Ibrutinib-MPEA Related Classifications
HY-43521 Related Classifications
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Keywords
- Ibrutinib-MPEA
- 1710768-30-1
- Target Protein Ligand-Linker Conjugates
- Btk
- STAT
- Bruton tyrosine kinase
- Bruton's tyrosine kinase
- primary mast cell tumour cells
- signal transducer and activator of transcription 5
- neoplastic mast cells
- cerebral ischemia/reperfusion injury
- BTK
- canine mast cell tumours
- STAT5
- neuroinflammation-related diseases
- diabetic mice
- Inhibitor
- inhibitor
- inhibit