Home Tools
Log in
Cart

BTK inhibitor 17

Catalog No. T9706   CAS 1858206-76-4

BTK inhibitor 17 is a potent irreversible BTK inhibitor (IC50 = 2.1 nM). BTK inhibitor 17 can be used in rheumatoid arthritis studies.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
BTK inhibitor 17 Chemical Structure
BTK inhibitor 17, CAS 1858206-76-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 175.00
5 mg In stock $ 372.00
10 mg In stock $ 556.00
25 mg In stock $ 896.00
50 mg In stock $ 1,220.00
100 mg In stock $ 1,650.00
1 mL * 10 mM (in DMSO) In stock $ 373.00
Bulk Inquiry
Get quote
Select Batch  
Purity: 99.57%
Purity: 99.29%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description BTK inhibitor 17 is a potent irreversible BTK inhibitor (IC50 = 2.1 nM). BTK inhibitor 17 can be used in rheumatoid arthritis studies.
Targets&IC50 BTK:2.1 nM
In vitro BTK inhibitor 17 exhibited high potency against BTK kinase and acceptable PK profile. BTK inhibitor 17 could covalently bind to Cys481 and formed an HB network with gatekeeper Thr474, hinge key residues Met477 and Glu475[1].
In vivo BTK inhibitor 17 demonstrated significant in vivo efficacy in a mouse-collagen-induced arthritis (CIA) model. BTK inhibitor 17 shows >95% plasma protein binding across three species of human, rat, and mouse. After an intravenous injection, the half-life (rat, 0.32 h; mice, 0.42 h), clearance (rat, 54.6 mL/min/kg; mice, 31.3 mL/min/kg), volume of distribution (rat, 1.55 L/kg; mice, 0.82 L/kg), and AUC exposure (rat, 604 ng.h/mL; mice, 576 ng.h/mL) are observed in two species. After oral administration, BTK inhibitor 17 exhibits higher Cmax (rat, 466 ng/mL; mice, 252 ng/mL) and plasma exposure (rat, 642 ng.h/mL; mice, 128 ng.h/mL) with a favorable oral bioavailability (rat, 23.7%; mice, 11.2%)[1]. In male Balb/C mice injected with collagen, BTK inhibitor 17 inhibited the significant progression of the disease and exhibited a clear dose-dependent reduction per paw clinical scores[1].
Molecular Weight 456.5
Formula C25H24N6O3
CAS No. 1858206-76-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (219.06 mM)

TargetMolReferences and Literature

1. Xuejun Zhang, et al. Discovery and Evaluation of Pyrazolo[3,4- d]pyridazinone as a Potent and Orally Active Irreversible BTK Inhibitor. ACS Med Chem Lett. 2019 Dec 11;11(10):1863-1868.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Angiogenesis related Compound Library Kinase Inhibitor Library Orally Active Compound Library Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max

Related Products

Related compounds with same targets
GDC-0834 JAK3/BTK-IN-1 BTK-IN-27 IBT6A PROTAC BTK Degrader-5 Btk inhibitor 2 Spebrutinib besylate Vecabrutinib

TargetMolDose Conversion

You can also refer to dose conversion for different animals. More

TargetMol In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

TargetMolCalculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BTK inhibitor 17 1858206-76-4 Angiogenesis Tyrosine Kinase/Adaptors BTK BTK inhibitor17 oral Btk rheumatoid Inhibitor inhibit Cys481 Bruton tyrosine kinase arthritis BTK inhibitor-17 inhibitor

 

TargetMol