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BMS-986195

Chemical Structure : BMS-986195

CAS No.: 1912445-55-6

BMS-986195 (BMS986195, Branebrutinib)

Catalog No.: PC-63295Not For Human Use, Lab Use Only.

BMS-986195 (Branebrutinib) is a novel potent, selective, covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK) with IC50 of 0.1 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BMS-986195 (Branebrutinib) is a novel potent, selective, covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK) with IC50 of 0.1 nM.
BMS-986195 (Branebrutinib) displays >5,000-fold selective over all kinases outside of the Tec family, and selectivity ranges 9- to 1010-fold within the Tec family.
BMS-986195 (Branebrutinib) potently inhibits antigen-dependent interleukin-6 production, CD86 expression and proliferation in B cells (IC50<1 nM).
BMS-986195 (Branebrutinib) demonstrates robust efficacy in murine models of RA including CIA and CAIA, protecting against clinically evident disease, histologic joint damage and bone mineral density loss.

Physicochemical Properties

M.Wt 370.428
Formula C20H23FN4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-4-(3-(but-2-ynamido)piperidin-1-yl)-5-fluoro-2,3-dimethyl-1H-indole-7-carboxamide

References

1. Watterson SH, et al. J Med Chem. 2019 Apr 11;62(7):3228-3250.
2. Catlett IM, et al. Br J Clin Pharmacol. 2020 Sep;86(9):1849-1859.
3. Wu CP, et al. Front Cell Dev Biol. 2021 Jul 19;9:699571.

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