2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. BIIB068

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.

For research use only. We do not sell to patients.

BIIB068 Chemical Structure

BIIB068 Chemical Structure

CAS No. : 1798787-27-5

Size Price Stock Quantity
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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 218 In-stock
Solution
10 mM * 1 mL in DMSO USD 218 In-stock
Solid
5 mg USD 198 In-stock
10 mg USD 330 In-stock
25 mg USD 605 In-stock
50 mg USD 1045 In-stock
100 mg USD 1815 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

BIIB068 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

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 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]
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]
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.

BIIB068 Related Antibodies
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 %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
Molecular Weight

435.52

Formula

C23H29N7O2
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2961 mL 11.4805 mL 22.9611 mL
5 mM 0.4592 mL 2.2961 mL 4.5922 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.69%

SDS (393 KB)

COA (245 KB) LCMS (94 KB)

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
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BIIB068 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BIIB0681798787-27-5BIIB 068BIIB-068BtkBruton tyrosine kinaseAutoimmunereversibleFcγRROSphosphorylationADMETNFαanti-IgManti-IgDInhibitorinhibitorinhibit

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