2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. BIIB091

BIIB091 is a potent, selective, orally active and reversible BTK inhibitor, with an IC50 of <0.5 nM. BIIB091 binds the BTK protein to sequester TYR-551 into an inactive conformation with excellent affinity. BIIB091 can be used for the research of multiple sclerosis.

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

BIIB091 Chemical Structure

BIIB091 Chemical Structure

CAS No. : 2247614-80-6

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1 mg USD 495 In-stock
5 mg USD 1090 In-stock
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25 mg USD 3680 In-stock
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Based on 1 publication(s) in Google Scholar

BIIB091 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

BIIB091 is a potent, selective, orally active and reversible BTK inhibitor, with an IC50 of <0.5 nM. BIIB091 binds the BTK protein to sequester TYR-551 into an inactive conformation with excellent affinity. BIIB091 can be used for the research of multiple sclerosis[1].

In Vitro

BIIB091 inhibits the phosphorylation of PLCγ2 in the Ramos human B-cell line, with an IC50 of 6.9 nM[1].
BIIB091 blocks anti-IgM-stimulated CD69 activation in PBMCs with an IC50 of 6.9 nM[1].
BIIB091 inhibits FcγR-induced ROS production in purified primary neutrophils, with an IC50 of 4.5 nM[1].
BIIB091 inhibits FcγRI and FcγRIII-mediated TNFα secretion upon simulation with FcγR agonists such as coated human IgG (all FcγR, IC50=5.6 nM), anti-CD16 (FcγRIII, IC50=8.0 nM), anti-CD64 (FcγRI IC50=3.1 nM), and cross-linked anti-CD16 (FcγRIII IC50=1.3 nM) in human monocytes[1].
BIIB091 inhibits the phosphorylation of BTK (IC50=24 nM) and blocks both BCR mediated B cell and FcεR-induced basophil activation as measured by inhibition of CD69 and CD63 expression (IC50=71 nM and IC50=82 nM, respectively) in the whole blood assays[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BIIB091 Related Antibodies
In Vivo

BIIB091 (0.03-30 mg/kg; p.o. twice daily for 10 d) reduces the anti-NP IgM antibody titers (88%, 77%, 59%, 59%, 44%, 34%, and 22%) in the TI-2 immunization model[1].

Pharmacokinetics of BIIB091 in preclinical species[1]

species IV (1 mg/kg) PO (5 mg/kg) in HMPC/Tween
T1/2 (h) AUCinf (h•ng/mL) CL (mL/min/kg) CL %QH Vdss (L/kg) Tmax (h) Cmax (ng/mL) AUCinf (h•ng/mL) %F
rat 2.1 748 10 22 0.4 0.9 693 1522 42
cyno 1.1 943 18 44 0.7 0.33 1104 1446 31
dog 6.0 1675 12 33 1.7 1.6 1440 6075 89

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice immunized with NP-Ficoll a thymus-independent type 2 (TI-2) antigen[1]
Dosage: 0.03, 0.1, 0.3, 1, 10, 30 mg/kg in a CMC/Tween suspension formulation
Administration: P.o. twice daily for 10 days
Result: Observed a significant reduction of the anti-NP IgM antibody titers (88%, 77%, 59%, 59%, 44%, 34%, and 22%).
Clinical Trial
Molecular Weight

542.64

Formula

C28H34N10O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CN(C(C)(C)C)N=N1)N[C@H]2C3=CC=C(C4=CC=NC(NC5=CN(C)N=C5)=N4)C=C3CN(C6COC6)CC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (230.36 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 1.8428 mL 9.2142 mL 18.4284 mL
5 mM 0.3686 mL 1.8428 mL 3.6857 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (3.83 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 (3.83 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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g

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(per animal)

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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: 99.85%

SDS (251 KB)

COA (255 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, 6 months; -20°C, 1 month. 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 1.8428 mL 9.2142 mL 18.4284 mL 46.0711 mL
5 mM 0.3686 mL 1.8428 mL 3.6857 mL 9.2142 mL
10 mM 0.1843 mL 0.9214 mL 1.8428 mL 4.6071 mL
15 mM 0.1229 mL 0.6143 mL 1.2286 mL 3.0714 mL
20 mM 0.0921 mL 0.4607 mL 0.9214 mL 2.3036 mL
25 mM 0.0737 mL 0.3686 mL 0.7371 mL 1.8428 mL
30 mM 0.0614 mL 0.3071 mL 0.6143 mL 1.5357 mL
40 mM 0.0461 mL 0.2304 mL 0.4607 mL 1.1518 mL
50 mM 0.0369 mL 0.1843 mL 0.3686 mL 0.9214 mL
60 mM 0.0307 mL 0.1536 mL 0.3071 mL 0.7679 mL
80 mM 0.0230 mL 0.1152 mL 0.2304 mL 0.5759 mL
100 mM 0.0184 mL 0.0921 mL 0.1843 mL 0.4607 mL
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BIIB091 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:

BIIB0912247614-80-6BIIB 091BIIB-091BtkBruton tyrosine kinaseInhibitorinhibitorinhibit

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