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BTK inhibitor 17

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Catalog No. T9706Cas No. 1858206-76-4

BTK inhibitor 17 is a potent irreversible Bruton’s tyrosine kinase (BTK) inhibitor with an IC50 value of 2.1 nM, suitable for use in rheumatoid arthritis studies.

BTK inhibitor 17

BTK inhibitor 17

🥰Excellent
Purity: 99.57%
Catalog No. T9706Cas No. 1858206-76-4
BTK inhibitor 17 is a potent irreversible Bruton’s tyrosine kinase (BTK) inhibitor with an IC50 value of 2.1 nM, suitable for use in rheumatoid arthritis studies.
Pack SizePriceAvailabilityQuantity
1 mg$86In Stock
5 mg$178In Stock
10 mg$278In Stock
25 mg$447In Stock
50 mg$592In Stock
100 mg$828In Stock
200 mg$1,090In Stock
1 mL x 10 mM (in DMSO)$178In Stock
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Purity:99.57%
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Product Introduction

Bioactivity
Description
BTK inhibitor 17 is a potent irreversible Bruton’s tyrosine kinase (BTK) inhibitor with an IC50 value of 2.1 nM, suitable for use 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].
Chemical Properties
Molecular Weight456.5
FormulaC25H24N6O3
Cas No.1858206-76-4
SmilesNc1n[nH]c(=O)c2n(nc(-c3ccc(Oc4ccccc4)cc3)c12)[C@@H]1CCCN(C1)C(=O)C=C
Relative Density.1.40 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (219.06 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1906 mL10.9529 mL21.9058 mL109.5290 mL
5 mM0.4381 mL2.1906 mL4.3812 mL21.9058 mL
10 mM0.2191 mL1.0953 mL2.1906 mL10.9529 mL
20 mM0.1095 mL0.5476 mL1.0953 mL5.4765 mL
50 mM0.0438 mL0.2191 mL0.4381 mL2.1906 mL
100 mM0.0219 mL0.1095 mL0.2191 mL1.0953 mL

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