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| | BMS-935177 Basic information |
| Product Name: | BMS-935177 | | Synonyms: | 9H-Carbazole-1-carboxamide, 7-(1-hydroxy-1-methylethyl)-4-[2-methyl-3-(4-oxo-3(4H)-quinazolinyl)phenyl]-;7-(2-Hydroxypropan-2-yl)-4-(2-methyl-3-(4-oxoquinazolin-3(4H)-yl)phenyl)-9H-carbazole-1-carboxamide;BMS 935177,BMS935177 | | CAS: | 1231889-53-4 | | MF: | C31H26N4O3 | | MW: | 502.56 | | EINECS: | | | Product Categories: | | | Mol File: | 1231889-53-4.mol |  |
| | BMS-935177 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 |
| | BMS-935177 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 | | 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 |
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| | BMS-935177 Preparation Products And Raw materials |
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