| Name | Branebrutinib |
| Description | Branebrutinib (BMS986195) is a potent, covalent inhibitor of Bruton's tyrosine kinase (BTK), >5,000-fold selective over all kinases outside of the Tec family (IC50 <1 nM for BTK). |
| In vitro | Branebrutinib inactivated BTK in human whole blood with a rapid rate of inactivation (3.5×10^-4 /nM/min) and potently inhibited antigen-dependent interleukin-6 production, CD86 expression and proliferation in B cells (IC50 <1 nM) without effect on antigen-independent measures in the same cells. A similar potency was measured against FcγR-dependent TNF-α production in human cells. |
| In vivo | In mice, a dose as low as 0.5 mg/kg, taken orally (PO) daily (QD), resulted in peak BTK inactivation of 98% after only the second dose. BTK was inactivated to similar levels in whole blood, lymph nodes and spleen in a dose-dependent manner. Branebrutinib demonstrated robust efficacy in murine models of RA including CIA and CAIA, protecting against clinically evident disease, histologic joint damage and bone mineral density loss. In both models, maximal efficacy was observed at doses ≤0.5 mg/kg PO QD, which achieved ≥95% inactivation of BTK in vivo. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (8.91 mM), Sonication is recommended.
DMSO : 100 mg/mL (269.96 mM), Sonication is recommended.
|
| Keywords | Inhibitor | inhibit | Btk | Bruton tyrosine kinase | Branebrutinib | BMS-986195 | BMS 986195 |
| Inhibitors Related | evobrutinib | (±)-Zanubrutinib | CP-547632 | CHMFL-EGFR-202 | Sunvozertinib | Ibrutinib | IBT6A | Orelabrutinib | Remibrutinib | Atuzabrutinib | Tyrosinase-IN-16 | Birelentinib |
| Related Compound Libraries | Nonsteroidal Anti-Inflammatory Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Drug Repurposing Compound Library | Angiogenesis related Compound Library | Inhibitor Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
