BMS-986142
- CAS No.
- 1643368-58-4
- Chemical Name:
- BMS-986142
- Synonyms
- BMS-986142;BMS-986142, 10 mM in DMSO;BMS-986142;BMS 986142;BMS986142;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;(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;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)-
- CBNumber:
- CB34667299
- Molecular Formula:
- C32H30F2N4O4
- Molecular Weight:
- 572.6
- MDL Number:
- MOL File:
- 1643368-58-4.mol
| 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) |
| form | A crystalline solid |
| pka | 15.03±0.29(Predicted) |
| color | White to off-white |
| FDA UNII | PJX9GH268R |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS07,GHS09 |
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|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| NFPA 704 |
|
BMS-986142 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Biosynth Carbosynth | BB170197 | BMS-986142 | 1643368-58-4 | 10mg | $175 | 2021-12-16 | Buy |
| AK Scientific | 5734EA | Bms-986142 | 1643368-58-4 | 10mg | $286 | 2021-12-16 | Buy |
| Biosynth Carbosynth | BB170197 | BMS-986142 | 1643368-58-4 | 50mg | $500 | 2021-12-16 | Buy |
| ChemScene | CS-0022067 | BMS-986142 99.92% | 1643368-58-4 | 5mg | $550 | 2021-12-16 | Buy |
| ChemScene | CS-0022067 | BMS-986142 99.92% | 1643368-58-4 | 10mg | $850 | 2021-12-16 | Buy |
BMS-986142 Chemical Properties,Uses,Production
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
Raw materials
Preparation Products
BMS-986142 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32268 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24727 | 58 |
| TargetMol Chemicals Inc. | support@targetmol.com | United States | 38663 | 58 | |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
| Suzhou ARTK Medchem Co., Ltd. | +86-512-68323658 +86-18168183658 | sales1@artkmedchem.com | China | 39002 | 58 |
| Wuhan Jingkang en Biomedical Technology Co., Ltd | +8613720134139 | orders@jknbiochem.com | China | 5221 | 58 |
View Lastest Price from BMS-986142 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2025-04-28 | BMS-986142
1643368-58-4
|
US $143.00-632.00 / mg | 99.76% | 10g | TargetMol Chemicals Inc. |
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- BMS-986142
1643368-58-4
- US $143.00-632.00 / mg
- 99.76%
- TargetMol Chemicals Inc.