PCI-33380
Based on 1 publication(s) in Google Scholar
PCI-33380 is a fluorescent probe ( (Ex=532 nm, Em=555 nm). PCI-33380 consists of a (BTK) inhibitor PCI-32765 (HY-10997) attaching with a Bodipy-FL fluorophore via a piperazine linker. PCI-33380 binds predominantly to Btk in B cell lysates with cell permeable activity. PCI-33380 can be used for imaging live cancer cells such as non-Hodgkin lymphoma research
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 1022899-36-0
- Formula: C46H52BF2N11O3
- Molecular Weight:855.78
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PCI-33380
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Biological Activity
PCI-33380 binds to Btk could be detected by denaturing gel electrophoresis and fluorescent gel scanning[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human B cells.
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Concentration:2 μM.
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Incubation Time:1 h.
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Result:Found that 10 nM of PCI-32765 was sufficient to fully occupy the active site of Btk in primary B cells in culture by using the fluorescently tagged derivative PCI-33380.
Chemical Information
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CAS No. 1022899-36-0
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Appearance Solid
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Molecular Weight 855.78
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Formula C46H52BF2N11O3
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Color Brown to red
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SMILES
NC1=C(C(C2=CC=C(OC3=CC=CC=C3)C=C2)=NN4C(CCC5)CN5C(/C=C/CN6CCN(CCNC(CCC7=CC=C(C=C(C(C)=C8)[N]9=C8C)[N-]7[B+3]9([F-])[F-])=O)CC6)=O)C4=NC=N1
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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 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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J Med Chem
Reinvent Aliphatic Arsenicals as Reversible Covalent Warheads toward Targeted Kinase Inhibition and Non-acute Promyelocytic Leukemia Cancer Treatment. [Abstract]2024 Apr 11;67(7):5458-5472. PMID: 38556750
Solvent & Solubility
DMSO : ≥ 50 mg/mL (58.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (2.92 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 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 (2.92 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.
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 (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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Zuo Y, et al. A novel 2,5-diaminopyrimidine-based affinity probe for Bruton's tyrosine kinase. Sci Rep. 2015 Nov 4;5:16136. [Content Brief]
[2]. Honigberg LA, et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci U S A. 2010 Jul 20;107(29):13075-80. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1685 mL | 5.8426 mL | 11.6852 mL | 29.2131 mL |
| 5 mM | 0.2337 mL | 1.1685 mL | 2.3370 mL | 5.8426 mL | |
| 10 mM | 0.1169 mL | 0.5843 mL | 1.1685 mL | 2.9213 mL | |
| 15 mM | 0.0779 mL | 0.3895 mL | 0.7790 mL | 1.9475 mL | |
| 20 mM | 0.0584 mL | 0.2921 mL | 0.5843 mL | 1.4607 mL | |
| 25 mM | 0.0467 mL | 0.2337 mL | 0.4674 mL | 1.1685 mL | |
| 30 mM | 0.0390 mL | 0.1948 mL | 0.3895 mL | 0.9738 mL | |
| 40 mM | 0.0292 mL | 0.1461 mL | 0.2921 mL | 0.7303 mL | |
| 50 mM | 0.0234 mL | 0.1169 mL | 0.2337 mL | 0.5843 mL |
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