| Identification | Back Directory | [Name]
BMS-935177 | [CAS]
1231889-53-4 | [Synonyms]
9H-Carbazole-1-carboxamide, 7-(1-hydroxy-1-methylethyl)-4-[2-methyl-3-(4-oxo-3(4H)-quinazolinyl)phenyl]- | [Molecular Formula]
C31H26N4O3 | [MDL Number]
MFCD30470964 | [MOL File]
1231889-53-4.mol | [Molecular Weight]
502.56 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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]
| Target | Value | BTK
(Cell-free assay) | 2.8 nM | TEC
(Cell-free assay) | 13 nM | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> BLK
(Cell-free assay) 20 nM | BMX
(Cell-free assay) | 24 nM | TrkA
(Cell-free assay) | 30 nM |
| [storage]
Store at -20°C |
|
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|