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
- Molecular Weight:
- 502.56
- MDL Number:
- MFCD30470964
- MOL File:
- 1231889-53-4.mol
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 price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
TRC | B596005 | BMS935177 | 1231889-53-4 | 5mg | $600 | 2021-12-16 | Buy |
TRC | B596005 | BMS935177 | 1231889-53-4 | 1mg | $190 | 2021-12-16 | Buy |
ChemScene | CS-0021905 | BMS-935177 99.33% | 1231889-53-4 | 5mg | $220 | 2021-12-16 | Buy |
ChemScene | CS-0021905 | BMS-935177 99.33% | 1231889-53-4 | 10mg | $350 | 2021-12-16 | Buy |
ChemScene | CS-0021905 | BMS-935177 99.33% | 1231889-53-4 | 2mg | $110 | 2021-12-16 | Buy |
BMS-935177 Chemical Properties,Uses,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) td> | 24 nM |
TrkA (Cell-free assay) | 30 nM |
BMS-935177 Preparation Products And Raw materials
Raw materials
Preparation Products
BMS-935177 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24738 | 58 |
Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43348 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Sichuan Wei Keqi Biological Technology Co., Ltd. | 028-81700200 18116577057 | 3003855609@qq.com | China | 7887 | 56 |
Mashilabs (Shanghai) Co.,Ltd. | 19916721580 | mafarm@126.com | China | 4115 | 58 |
Shanghaizehan biopharma technology co., Ltd. | 021-61350663 13052117465 | sales@zehanbiopharma.com | China | 998 | 55 |