Art. -Nr.: HY-131342

BIIB068

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BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC₅₀ of 1 nM and a K_d 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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Reinheit: 98.35%
CAS. Nr.: 1798787-27-5
Formel: C₂₃H₂₉N₇O₂
Molecular Weight:435.52

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

BIIB068 Chemical Structure

CAS. Nr.: 1798787-27-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 1 nM (BTK)^[1]
Kd: 0.3 nM (BTK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	>20 μM Compound: 1; BIIB068	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	[PMID: 32696648]
PBMC	IC₅₀	>10 μM Compound: 1; BIIB068	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	[PMID: 32696648]
PBMC	IC₅₀	>10 μM Compound: 1; BIIB068	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	[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.

In Vivo

BIIB068 (compound 1) is stable in the plasma of mouse, rat, beagle dog, and cynomolgus monkey (>95% parent compound remaining after 6 hours of incubation)^[1].
BIIB068 (compound 1) exhibits good drug-like properties (LLE = 5) which results in low in vivo clearance (CL %Q_h = 6) and moderate oral bioavailability (%F = 48) when dosed in rats. BIIB068 (5 mg/kg; po) treatment shows the T_1/2 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 A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1798787-27-5
Appearance Solid
Molecular Weight 435.52
Formel C₂₃H₂₉N₇O₂
Color Off-white to yellow
SMILES

O=C(N1CC(OC(C)C)C1)NCC2=CC=C(C3=NC(NC4=CN(C)N=C4)=NC=C3)C=C2C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2961 mL

11.4805 mL

22.9611 mL

5 mM

0.4592 mL

2.2961 mL

4.5922 mL

10 mM

0.2296 mL

1.1481 mL

2.2961 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Bin Ma, Tonika Bohnert, et al. Discovery of BIIB068: A Selective, Potent, Reversible Bruton's Tyrosine Kinase Inhibitor as an Orally Efficacious Agent for Autoimmune Diseases. J Med Chem. 2020 Jul 22. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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BIIB068

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Clinical Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BIIB068

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Clinical Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BIIB068 Related Classifications

HY-131342 Related Classifications