Branebrutinib

SKU: orb1301816

Description

Branebrutinib (BMS-986195) is a highly selective, covalent Bruton's tyrosine kinase (BTK) inhibitor with sub-nanomolar potency. Its >5,000-fold selectivity over kinases outside the Tec family makes it a valuable tool for investigating BTK-dependent signaling in autoimmune and oncology research, applicable in both cellular and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	1912445-55-6
MW	370.42
Purity	99.39% (May vary between batches)
Formula	C₂₀H₂₃FN₄O₂
SMILES	CC#CC(=O)N[C@H]1CCCN(C1)c1c(F)cc(C(N)=O)c2[nH]c(C)c(C)c12
Target	BTK
Solubility	DMSO:100 mg/mL (269.96 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (8.91 mM)

Bioactivity

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Target IC50	BTK:<1 nM (cell free)
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. Read more...
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. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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BTK, Btk, BMS 986195, BMS986195, BMS-986195, Branebrutinib, Bruton tyrosine kinase, inhibit, Inhibitor

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Compound Identifiers

PubChem CID

121293929 ↗

Key Properties

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No computed properties available.

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Branebrutinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

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Protocol Information

Branebrutinib (orb1301816)

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