| Name | BTK inhibitor 17 |
| 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. |
| 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 100 mg/mL (219.06 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (8.76 mM), Sonication is recommended.
|
| Keywords | rheumatoid | oral | Inhibitor | inhibit | Cys481 | BTK inhibitor-17 | BTK inhibitor17 | BTK inhibitor 17 | Btk | Bruton tyrosine kinase | arthritis |
| Inhibitors Related | evobrutinib | (±)-Zanubrutinib | CP-547632 | CHMFL-EGFR-202 | Sunvozertinib | Ibrutinib | IBT6A | Orelabrutinib | Remibrutinib | Atuzabrutinib | Tyrosinase-IN-16 | Birelentinib |
| Related Compound Libraries | Cysteine Covalent Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Angiogenesis related Compound Library | Inhibitor Library | Orally Active Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-Cancer Compound Library |
United States
