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BMS-986142

Catalog No. T5138 CAS 1643368-58-4

BMS-986142 is a potent and highly selective reversible BTK inhibitor (IC50: 0.5 nM).

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BMS-986142, CAS 1643368-58-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 143.00
5 mg	In stock	$ 397.00
10 mg	In stock	$ 632.00
25 mg	In stock	$ 989.00
50 mg	In stock	$ 1,330.00
100 mg	In stock	$ 1,780.00
200 mg	In stock	$ 2,430.00
500 mg	In stock	$ 3,590.00
1 mL * 10 mM (in DMSO)	In stock	$ 513.00

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Purity: 99.76%

Purity: 99.13%

Purity: 98.7%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	BMS-986142 is a potent and highly selective reversible BTK inhibitor (IC50: 0.5 nM).
Targets&IC50	BLK:23 nM (cell free), BTK:0.5 nM (cell free), TXK:28 nM (cell free), BMX:32 nM (cell free), ITK:15 nM (cell free), TEC:10 nM (cell free)
In vitro	Against a panel of 384 kinases, BMS-986142 is highly selective, with only five other kinases (Tec, ITK, BLK, Txk, BMX) inhibited with <100-fold selectivity for BTK. Four of these kinases are Tec family kinases, of which BTK is a member, and only Tec (IC50: 10 nM) is inhibited with <30-fold selectivity compared with BTK. BMS-986142 does not inhibit CD40L-induced expression of CD86 or CD69 on peripheral blood B cells (IC50>10,000 nM for both). When Ramos B cells are treated with anti-IgM to activate BCR, BMS-986142 inhibits BTK-dependent calcium flux (IC50: 9 nM) [2].
In vivo	BMS-986142 administration at doses of 4, 10, and 30 mg/kg produces dose-dependent decreases in clinically evident disease by 26%, 43%, and 79%, respectively. Notably, at a 4 mg/kg dose, BMS-986142, when used in conjunction with MTX, enhances clinical scores by achieving a 54% inhibition, compared to a 19% inhibition with MTX alone. Further, this co-administration at 4 mg/kg leads to a 53% reduction in inflammation and bone resorption, significantly more effective than the 24% and 10% reductions observed with each drug individually. Additionally, serum anti-collagen II IgG levels are notably reduced with 10 and 30 mg/kg doses of BMS-986142. The compound also demonstrates efficacy in delayed treatment protocols, showing dose-dependent improvements in clinical scores even when administration begins on day 21, with 2, 4, and 25 mg/kg doses resulting in clinical score reductions of 17%, 37%, and 67%, respectively, by study's end [2].
Animal Research	Male DBA/1 mice are injected subcutaneously at the base of the tail with bovine type II collagen (200 μg) admixed. The mice are boosted 21 days later in the same manner. For preventative administration, PO QD dosing is immediately started with BMS-986142 in EtOH: TPGS: PEG300 (5:5:90); for therapeutic administration, the start of dosing is delayed until the booster immunization on day 21. For BMS-986142 plus MTX preventative studies, mice receive vehicle; BMS-986142 at 4, 10, or 30 mg/kg; BMS-986142 at 4 mg/kg plus MTX 0.25 mg/kg; or MTX at 0.25 mg/kg daily. For BMS-986142 plus etanercept therapeutic studies, mice receive vehicle daily; BMS-986142 at 2, 4, or 25 mg/kg daily; BMS-986142 at 2 or 4 mg/kg daily plus etanercept at 15 mg/kg IP twice weekly (BIW); or etanercept at 15 mg/kg IP BIW. For BMS-986142 plus murine cytotoxic T lymphocyte-associated protein 4 immunoglobulins (CTLA-4-Ig) preventative studies, mice receive vehicle daily; BMS-986142 at 10 or 30 mg/kg daily; murine CTLA-4-Ig at 0.05 or 0.2 mg/kg IP BIW; or BMS-986142 at 10 mg/kg daily plus murine CTLA-4-Ig at 0.05 or 0.2 mg/kg IP BIW. Dosing proceeds from day 0 through study completion (36 days).

Molecular Weight	572.6
Formula	C32H30F2N4O4
CAS No.	1643368-58-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 120 mg/mL

H2O: Insoluble

References and Literature

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-1986142): 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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Tyrosine Kinase Inhibitor Library Drug Repurposing Compound Library Highly Selective Inhibitor Library Immuno-Oncology Compound Library Target-Focused Phenotypic Screening Library Angiogenesis related Compound Library Kinase Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library

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RN486 BMS-935177 XMU-MP-2 N-piperidine Ibrutinib hydrochloride BTK-IN-16 AS-1763 Spebrutinib besylate Rilzabrutinib

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Keywords

BMS-986142 1643368-58-4 Angiogenesis Tyrosine Kinase/Adaptors BTK Btk inhibit BMS 986142 Inhibitor Bruton tyrosine kinase BMS986142 inhibitor

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