Atuzabrutinib
Based on 1 Customer Validation
Atuzabrutinib (SAR 444727) is a potent, selective reversible inhibitor of Btk (Bruton's tyrosine kinase) inhibitor. Atuzabrutinib inhibits neutrophil recruitment via inhibition of macrophage antigen-1 signalling.
For research use only. We do not sell to patients.
- Purity: 98.00%
- CAS No.: 1581714-49-9
- Formula: C30H30FN7O2
- Molecular Weight:539.60
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B cell | IC50 |
216 nM
Compound: 11; PRN473
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Inhibition of anti-IgM-stimulated CD20+ B cell activation in human whole blood assessed as measuring CD69 expression level pretreated for 1 hr followed by anti-IgM stimulation measured after 18 hrs by flow cytometry
Inhibition of anti-IgM-stimulated CD20+ B cell activation in human whole blood assessed as measuring CD69 expression level pretreated for 1 hr followed by anti-IgM stimulation measured after 18 hrs by flow cytometry
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[PMID: 35302767] |
| T-cell | IC50 |
>5 μM
Compound: 11; PRN473
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Inhibition of IL-2 production in TCR-stimulated T-cells in human whole blood
Inhibition of IL-2 production in TCR-stimulated T-cells in human whole blood
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[PMID: 35302767] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1581714-49-9
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Appearance Solid
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Molecular Weight 539.60
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Formula C30H30FN7O2
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Color White to off-white
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SMILES
NC1=C2C(N([C@H]3CN(CCC3)C(/C(C#N)=C/C(C)(C)C)=O)N=C2C4=C(C=C(C=C4)OC5=CC=CC=C5)F)=NC=N1
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Synonyms
SAR 444727; PRN473
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 100 mg/mL (185.32 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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 (278 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 (sealed storage, away from moisture and light). 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 | 1.8532 mL | 9.2661 mL | 18.5322 mL | 46.3306 mL |
| 5 mM | 0.3706 mL | 1.8532 mL | 3.7064 mL | 9.2661 mL | |
| 10 mM | 0.1853 mL | 0.9266 mL | 1.8532 mL | 4.6331 mL | |
| 15 mM | 0.1235 mL | 0.6177 mL | 1.2355 mL | 3.0887 mL | |
| 20 mM | 0.0927 mL | 0.4633 mL | 0.9266 mL | 2.3165 mL | |
| 25 mM | 0.0741 mL | 0.3706 mL | 0.7413 mL | 1.8532 mL | |
| 30 mM | 0.0618 mL | 0.3089 mL | 0.6177 mL | 1.5444 mL | |
| 40 mM | 0.0463 mL | 0.2317 mL | 0.4633 mL | 1.1583 mL | |
| 50 mM | 0.0371 mL | 0.1853 mL | 0.3706 mL | 0.9266 mL | |
| 60 mM | 0.0309 mL | 0.1544 mL | 0.3089 mL | 0.7722 mL | |
| 80 mM | 0.0232 mL | 0.1158 mL | 0.2317 mL | 0.5791 mL | |
| 100 mM | 0.0185 mL | 0.0927 mL | 0.1853 mL | 0.4633 mL |