Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor。The IC50 of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease.
| Molecular Weight | 297.35 |
| Formula | C17H19N3O2 |
| CAS Number | 1643570-24-4 |
| Form | Solid |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related BTK Products |
|---|
| TL-925
TL-925 is a potentially first-in-class Bruton's tyrosine kinase (BTK) inhibitor that targets mast cell-mediated ocular inflammation and hypersensitivity and can be used in studies related to dry eye. |
| JAK3/BTK-IN-6
JAK3/BTK-IN-6 is a potent BTK and JAK3 dual inhibitor, with IC50 values of 0.6 and 0.4 nM, respectively. |
| NX-2127
NX-2127 is an orally active, potent BTK inhibitor that induces degradation of mutant BTKC481S in cells, as well as inhibits the proliferation of BTKC481S mutant TMD8 cells. In addition, NX-2127 stimulates T cell activation and increases IL-2 production in primary human T cells. |
| DBt-10
DBt-10 is a potent BTK degrader. |
| BTK-IN-27
BTK-IN-27 is a BTK inhibitor (IC50: 0.2 nM). |
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