BMS-935177

Product NameBMS-935177
CAS1231889-53-4
MFC31H26N4O3
MW502.56
EINECS
MOL File1231889-53-4.mol

Chemical Properties

Boiling point	805.4±75.0 °C(Predicted)
Density	1.35±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO:115.0(Max Conc. mg/mL);228.82(Max Conc. mM) Ethanol:100.0(Max Conc. mg/mL);198.98(Max Conc. mM)
form	Solid
pka	14.45±0.29(Predicted)
color	Light yellow to yellow

Usage And Synthesis

Uses

BMS 935177 is a potent and selective reversible inhibitor of Bruton’s tyrosine kinase (Btk) with an IC50 of 3 nM.

Biological Activity

BMS-935177 is a potent and reversible BTK inhibitor with IC50 of 2.8 nM and good kinase selectivity. It is more potent and 5-67 times more selective against BTK than other kinases such as TEC, BMX, ITK, and TXK.

in vitro

BMS-935177 is more than 50-fold selective for BTK over SRC kinase family members. In Ramos B cells, it inhibits calcium flux; in peripheral blood B lymphocytes stimulated with anti-IgM and anti-IgG, it inhibits the cell surface expression of CD69. However, BMS-935177 had no effect on CD69 expression in B cells stimulated by CD40 receptor and ligand. In PBMCs, it can effectively inhibit the production of TNF-α with IC50 of 14 nM.

in vivo

Among the various tested species, BMS-935177 is highly bound to plasma proteins, with a free drug ratio of less than 1% in humans. In preclinical tests, it had good oral activity whether administered as a suspension or solution, despite its poor water solubility. When administered in solution, it has an oral bioavailability of 84%-100% in rats, mice, dogs, and cynomolgus monkeys, while in a single intravenous administration experiment, it has a lower in vivo bioavailability clearance rate. The T_1/2 of it was 4 h and 5.1 h by intravenous injection in mice and rats at a dose of 2 mg/kg, respectively.

target

< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> BLK
(Cell-free assay)

Target	Value
BTK (Cell-free assay)	2.8 nM
TEC (Cell-free assay)	13 nM
20 nM
BMX (Cell-free assay)	24 nM
TrkA (Cell-free assay)	30 nM

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