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Branebrutinib

Cat. No. M9628

All AbMole products are for research use only, cannot be used for human consumption.

Branebrutinib Structure
Synonym:

BMS-986195

Size Price Availability Quantity
5mg USD 155  USD155 In stock
10mg USD 230  USD230 In stock
25mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

Branebrutinib (BMS-986195) is a potent, covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), with IC50 of 0.1 nM. BMS-986195 is more than 5000-fold selective for BTK over all kinases outside of the Tec family, and selectivity ranges from 9- to 1010-fold within the Tec family. BMS-986195 inactivated BTK in human whole blood with a rapid rate of inactivation (3.5×10-4 nM-1·min-1) 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. In multi-species pharmacokinetic studies, the absolute oral bioavailability of BMS-986195 is 100% in mice, 74% in rats, 46% in cynomolgus monkeys, and 81% in dogs. The total body plasma clearance of BMS-986195 is low in all species.

Chemical Information
Molecular Weight 370.42
Formula C20H23FN4O2
CAS Number 1912445-55-6
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Scott H Watterson, et al. J Med Chem. Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK)

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Keywords: Branebrutinib, BMS-986195 supplier, BTK, inhibitors, activators

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