BMS-986142 manufacturers
- BMS-986142
-
- $113.00 / 1mg
-
2026-03-13
- CAS:1643368-58-4
- Min. Order:
- Purity: 99.44%
- Supply Ability: 10g
|
| | BMS-986142 Basic information |
| Product Name: | BMS-986142 | | Synonyms: | BMS-986142;BMS-986142;BMS 986142;BMS986142;1H-Carbazole-8-carboxamide, 6-fluoro-5-[(3S)-3-(8-fluoro-1,4-dihydro-1-methyl-2,4-dioxo-3(2H)-quinazolinyl)-2-methylphenyl]-2,3,4,9-tetrahydro-2-(1-hydroxy-1-methylethyl)-, (2S,5R)-;(2S,5R)-6-fluoro-5-[(3S)-3-(8-fluoro-1,4-dihydro-1-methyl-2,4-dioxo-3(2H)-quinazolinyl)-2-methylphenyl]-2,3,4,9-tetrahydro-2-(1-hydroxy-1-methylethyl)-1H-Carbazole-8-carboxamide;Btk,BMS-986142,inhibit,BMS986142,Inhibitor,Bruton tyrosine kinase,BMS 986142;(2S,5R)-6-Fluoro-5-((3S)-3-(8-fluoro-1-methyl-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)-2-methylphenyl)-2-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide;BMS-986142, 10 mM in DMSO;BMS-986142 (BMS 986142 | | CAS: | 1643368-58-4 | | MF: | C32H30F2N4O4 | | MW: | 572.6 | | EINECS: | | | Product Categories: | | | Mol File: | 1643368-58-4.mol |  |
| | BMS-986142 Chemical Properties |
| Boiling point | 746.5±70.0 °C(Predicted) | | density | 1.394±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO:76.67(Max Conc. mg/mL);133.9(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:3):0.25(Max Conc. mg/mL);0.44(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);52.39(Max Conc. mM)
Ethanol:15.0(Max Conc. mg/mL);26.2(Max Conc. mM) | | pka | 15.03±0.29(Predicted) | | form | A crystalline solid | | color | White to off-white | | InChIKey | ZRYMMWAJAFUANM-UHFFFAOYSA-N | | SMILES | FC1=CC(C(=O)N)=C2NC3CC(C(O)(C)C)CCC=3C2=C1C1C=CC=C(N2C(N(C)C3=C(C=CC=C3C2=O)F)=O)C=1C |
| | BMS-986142 Usage And Synthesis |
| Uses | BMS-986142 is a potent and highly selective reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.5 nM. | | in vivo | BMS-986142 at 4, 10, and 30 mg/kg results in dose-dependent reductions of 26%, 43%, and 79% in clinically evident disease, respectively, at the end of the study. Interestingly, 4 mg/kg BMS-986142 provides an additive benefit in clinical scores (54% inhibition) when co-administered with MTX versus 19% inhibition with MTX alone. Co-administration of BMS-986142 at 4 mg/kg with MTX result in a 53% reduction in inflammation and bone resorption compared with 24% and 10%, respectively, with either drug alone. Furthermore, serum anti-collagen II IgG titers are significantly inhibited with 10 and 30 mg/kg BMS-986142. BMS-986142 also produces dose-dependent reductions in clinical scores when administration is delayed until the collagen booster on day 21. BMS-986142 doses of 2, 4, and 25 mg/kg in this therapeutic dosing regimen result in clinical score reductions of 17%, 37%, and 67%, respectively, at the end of the study[2]. | | References | [1] Watterson SH, et al. Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers. J Med Chem. 2016 Oct 13;59(19):9173-9200.
[2] Kathleen M. Gillooly, et al. Bruton'styrosine kinase inhibitor BMS-986142 in experimental models of rheumatoid arthritis enhances efficacy of agents representing clinical standard-of-care. PLoS One. 2017; 12(7): e0181782. DOI:10.1371/journal.pone.0181782 |
| | BMS-986142 Preparation Products And Raw materials |
|