Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 54.00 | |
2 mg | In stock | $ 80.00 | |
5 mg | In stock | $ 153.00 | |
10 mg | In stock | $ 233.00 | |
25 mg | In stock | $ 393.00 | |
50 mg | In stock | $ 583.00 | |
100 mg | In stock | $ 835.00 | |
200 mg | In stock | $ 1,150.00 | |
500 mg | In stock | $ 1,690.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 153.00 |
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). |
Targets&IC50 | BTK:<1 nM (cell free) |
In vitro | BMS-986195 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. BMS-986195 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. |
Synonyms | BMS986195 |
Molecular Weight | 370.42 |
Formula | C20H23FN4O2 |
CAS No. | 1912445-55-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (269.96 mM)
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Branebrutinib 1912445-55-6 Angiogenesis Tyrosine Kinase/Adaptors BTK Inhibitor Btk BMS986195 BMS 986195 inhibit Bruton tyrosine kinase BMS-986195 inhibitor