BIIB068
Based on 1 Customer Validation
BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC50 of 1 nM and a Kd of 0.3 nM. BIIB068 shows more >400-fold selective for BTK than other kinases. BIIB068 has the potential for autoimmune diseases research.
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- Purity : 98.35%
- CAS No.: 1798787-27-5
- 화학식: C23H29N7O2
- 분자량:435.52
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
>20 μM
Compound: 1; BIIB068
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Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 24 hrs by via-light reagent based ATP bioluminescence assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 24 hrs by via-light reagent based ATP bioluminescence assay
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[PMID: 32696648] |
| PBMC | IC50 |
>10 μM
Compound: 1; BIIB068
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Inhibition of anti-CD3/anti-CD28-induced T cell activation in human PBMC preincubated for 30 mins followed by anti-CD3/anti-CD28 stimulation and measured after 18 to 22 hrs by CD4-APC-H7/CD8-FITC/CD2-PE-Cy7/CD19-APC and CD69-PE staining based flow cytomet
Inhibition of anti-CD3/anti-CD28-induced T cell activation in human PBMC preincubated for 30 mins followed by anti-CD3/anti-CD28 stimulation and measured after 18 to 22 hrs by CD4-APC-H7/CD8-FITC/CD2-PE-Cy7/CD19-APC and CD69-PE staining based flow cytomet
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[PMID: 32696648] |
| PBMC | IC50 |
>10 μM
Compound: 1; BIIB068
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Inhibition of IL-4/anti-CD40/CD40-induced B cell activation in human PBMC preincubated for 30 mins followed by anti-human CD40 mAb/recombinant human IL-4 stimulation and measured after 18 to 22 hrs by CD19-APC/CD69-PE staining based flow cytometry
Inhibition of IL-4/anti-CD40/CD40-induced B cell activation in human PBMC preincubated for 30 mins followed by anti-human CD40 mAb/recombinant human IL-4 stimulation and measured after 18 to 22 hrs by CD19-APC/CD69-PE staining based flow cytometry
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[PMID: 32696648] |
In Vitro
BIIB068 (compound 1) improves the whole blood cell potency (human whole blood BTK phosphorylation (IC50 = 0.12 µM)[1].
BIIB068 (compound 1; 30 µM,10 µM, 3.3 µM, and 1.1 µM) inhibits BCR mediated PLCγ2 phosphorylation in Ramos B cells (IC50= 0.4 µM), anti-IgD induced and anti-IgM BCR-induced B cell activation in human PBMCs (IC50 = 0.11 µM and 0.21 µM, respectively)[1].
BIIB068 (compound 1) inhibits FcγR-mediated ROS production in neutrophils with an IC50 of 54 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
BIIB068 (compound 1) exhibits good drug-like properties (LLE = 5) which results in low in vivo clearance (CL %Qh = 6) and moderate oral bioavailability (%F = 48) when dosed in rats. BIIB068 (5 mg/kg; po) treatment shows the T1/2 of 1.2 hours, 2.1 hours and 0.9 hour for rats, dog and cynomolgus monkey, respectively. BIIB068 shows acceptable ADME (absorption, distribution, metabolism, and excretion) properties[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1798787-27-5
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Appearance Solid
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분자량 435.52
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화학식 C23H29N7O2
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Color Off-white to yellow
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SMILES
O=C(N1CC(OC(C)C)C1)NCC2=CC=C(C3=NC(NC4=CN(C)N=C4)=NC=C3)C=C2C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
In Vitro:
DMSO : 31.25 mg/mL (71.75 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, 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)
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: ≥ 2.08 mg/mL (4.78 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 (4.78 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.
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.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
순도&문서
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Data Sheet (270 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, 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 | 2.2961 mL | 11.4805 mL | 22.9611 mL | 57.4026 mL |
| 5 mM | 0.4592 mL | 2.2961 mL | 4.5922 mL | 11.4805 mL | |
| 10 mM | 0.2296 mL | 1.1481 mL | 2.2961 mL | 5.7403 mL | |
| 15 mM | 0.1531 mL | 0.7654 mL | 1.5307 mL | 3.8268 mL | |
| 20 mM | 0.1148 mL | 0.5740 mL | 1.1481 mL | 2.8701 mL | |
| 25 mM | 0.0918 mL | 0.4592 mL | 0.9184 mL | 2.2961 mL | |
| 30 mM | 0.0765 mL | 0.3827 mL | 0.7654 mL | 1.9134 mL | |
| 40 mM | 0.0574 mL | 0.2870 mL | 0.5740 mL | 1.4351 mL | |
| 50 mM | 0.0459 mL | 0.2296 mL | 0.4592 mL | 1.1481 mL | |
| 60 mM | 0.0383 mL | 0.1913 mL | 0.3827 mL | 0.9567 mL |
BIIB068 Related Classifications
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