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Remibrutinib (LOU064) is a potent and highly selective covalent Inhibitor of Bruton's Tyrosine Kinase (BTK) with IC50 value of 1 nM. LOU064 (Remibrutinib) exhibits an exquisite kinase selectivity due to binding to an inactive conformation of BTK and has the potential for a best-in-class covalent BTK inhibitor for the treatment of autoimmune diseases. LOU064 (Remibrutinib) demonstrates potent in vivo target occupancy with an EC90 of 1.6 mg/kg and dose-dependent efficacy in rat collagen-induced arthritis.
| Cell Experiment | |
|---|---|
| Cell lines | human monocytic cell line THP1, Human Blood B cell and Basophil |
| Preparation method | The effects of LOU064 on signaling from the activating FcγR are assessed in the human monocytic cell line THP1 (ATCC, TIB-202). The THP1 cell line expresses the two activating FcγRs CD32a (FcγRII2) and CD64 (FcγRI) that signal through BTK. Briefly, 384 well culture plates are coated with pooled non-specific human IgG fraction. Serial compound dilutions are dispensed into the IgG-coated plates containing a small volume of tissue culture medium. Then THP1 cells that are pre-differentiated by vitamin D3 treatment for 5 days are added to each well. Twenty-four hours later the secretion of IL-8 in the supernatant of these culture wells is assessed by a homogenous immunoassay. |
| Concentrations | 3 nM, 10 nM, 30 nM, 100 nM, 300 nM |
| Incubation time | 25 min, 50 min, 75 min, 100 min |
| Animal Experiment | |
|---|---|
| Animal models | Female Lewis rats, female C57BL/6 mice, male beagle dog |
| Formulation | - |
| Dosages | 1 mg/kg, 3 mg/kg |
| Administration | i.v. or p.o. administration |
| Molecular Weight | 507.53 |
| Formula | C27H27F2N5O3 |
| CAS Number | 1787294-07-8 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related BTK Products |
|---|
| PCI-32765
PCI-32765 (Ibrutinib) is a potent, selective and orally bioavailable irreversible inhibitor of BTK with IC50 value of 0.46 nM. |
| Spebrutinib (AVL-292)
Spebrutinib (AVL-292) is an oral, potent and selective small molecule covalent inhibitor of Btk (IC50 < 0.5 nM). |
| CNX-774
CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM. |
| GDC-0834
GDC-0834 is a novel potent and selective BTK inhibitor with IC50 of 5.9 nM. |
| CGI1746
CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM. |
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