BMS-935177
- Product Name
- BMS-935177
- CAS No.
- 1231889-53-4
- Chemical Name
- BMS-935177
- Synonyms
- BMS 935177,BMS935177;7-(2-Hydroxypropan-2-yl)-4-(2-methyl-3-(4-oxoquinazolin-3(4H)-yl)phenyl)-9H-carbazole-1-carboxamide;9H-Carbazole-1-carboxamide, 7-(1-hydroxy-1-methylethyl)-4-[2-methyl-3-(4-oxo-3(4H)-quinazolinyl)phenyl]-
- CBNumber
- CB23378977
- Molecular Formula
- C31H26N4O3
- Formula Weight
- 502.56
- MOL File
- 1231889-53-4.mol
BMS-935177 Property
- 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) - pka
- 14.45±0.29(Predicted)
N-Bromosuccinimide Price
- Product number
- B596005
- Product name
- BMS935177
- Packaging
- 5mg
- Price
- $600
- Updated
- 2021/12/16
- Product number
- B596005
- Product name
- BMS935177
- Packaging
- 1mg
- Price
- $190
- Updated
- 2021/12/16
- Product number
- CS-0021905
- Product name
- BMS-935177
- Purity
- 99.33%
- Packaging
- 5mg
- Price
- $220
- Updated
- 2021/12/16
- Product number
- CS-0021905
- Product name
- BMS-935177
- Purity
- 99.33%
- Packaging
- 10mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0021905
- Product name
- BMS-935177
- Purity
- 99.33%
- Packaging
- 2mg
- Price
- $110
- Updated
- 2021/12/16
BMS-935177 Chemical Properties,Usage,Production
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 |
| 20 nM | |
| BMX (Cell-free assay) | 24 nM |
| TrkA (Cell-free assay) | 30 nM |
BMS-935177 Preparation Products And Raw materials
Raw materials
Preparation Products
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