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Branebrutinib

🥰Excellent
Catalog No. T5407Cas No. 1912445-55-6
Alias BMS986195

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).

Branebrutinib

Branebrutinib

🥰Excellent
Purity: 99.39%
Catalog No. T5407Alias BMS986195Cas No. 1912445-55-6
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 SizePriceAvailabilityQuantity
1 mg51 €In Stock
2 mg76 €In Stock
5 mg145 €In Stock
10 mg221 €In Stock
25 mg373 €In Stock
50 mg553 €In Stock
100 mg793 €In Stock
200 mg1.092 €In Stock
500 mg1.605 €In Stock
1 mL x 10 mM (in DMSO)145 €In Stock
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Purity:99.39%
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Product Introduction

Bioactivity
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
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.
AliasBMS986195
Chemical Properties
Molecular Weight370.42
FormulaC20H23FN4O2
Cas No.1912445-55-6
SmilesCC#CC(=O)N[C@H]1CCCN(C1)c1c(F)cc(C(N)=O)c2[nH]c(C)c(C)c12
Relative Density.1.32 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (269.96 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6996 mL13.4982 mL26.9964 mL134.9819 mL
5 mM0.5399 mL2.6996 mL5.3993 mL26.9964 mL
10 mM0.2700 mL1.3498 mL2.6996 mL13.4982 mL
20 mM0.1350 mL0.6749 mL1.3498 mL6.7491 mL
50 mM0.0540 mL0.2700 mL0.5399 mL2.6996 mL
100 mM0.0270 mL0.1350 mL0.2700 mL1.3498 mL

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