ChemicalBook > CAS DataBase List > BMS-986142

BMS-986142

Product Name: BMS-986142
CAS No.: 1643368-58-4
Chemical Name: BMS-986142
Synonyms: BMS-986142;BMS-986142 (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
Formula Weight: 572.6
MOL File: 1643368-58-4.mol

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BMS-986142 Property

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
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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Warning

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N-Bromosuccinimide Price

Biosynth Carbosynth

Product number: BB170197
Product name: BMS-986142
Packaging: 10mg
Price: $175
Updated: 2021/12/16

AK Scientific

Product number: 5734EA
Product name: Bms-986142
Packaging: 10mg
Price: $286
Updated: 2021/12/16

Biosynth Carbosynth

Product number: BB170197
Product name: BMS-986142
Packaging: 50mg
Price: $500
Updated: 2021/12/16

ChemScene

Product number: CS-0022067
Product name: BMS-986142
Purity: 99.92%
Packaging: 5mg
Price: $550
Updated: 2021/12/16

ChemScene

Product number: CS-0022067
Product name: BMS-986142
Purity: 99.92%
Packaging: 10mg
Price: $850
Updated: 2021/12/16

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BMS-986142 Chemical Properties,Usage,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

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1643368-58-4, BMS-986142Related Search:

BMS-986020 BMS-852927 XL-652 BMS 303141 BMS813160 2-Piperidinecarboxylic acid, 1-[[2,6-dimethoxy-4-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]phenyl]methyl]-, (2S)- Insulin-like Growth Factor-1 Receptor Inhibitor PD-L1 inhibitor 1 AC480 (BMS-599626) BMS-986205

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

1643368-58-4

C32H30F2N4O4