[CAS NO. 1643368-58-4]  BMS-986142

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PRODUCTS SPECIFICATIONS [1643368-58-4]

Catalog
SLK-S8381
Brand
Selleck
CAS
1643368-58-4

DESCRIPTION [1643368-58-4]

Overview

MDL-
Molecular Weight572.60
Molecular FormulaC32H30F2N4O4
SMILESO=C(C1=CC(F)=C(C2=CC=CC(N3C(N(C)C4=C(C=CC=C4F)C3=O)=O)=C2C)C5=C1NC6=C5CC[C@H](C(C)(O)C)C6)N

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

BMS-986142 is a potent and highly selective reversible small molecule inhibitor of BTK with an IC50 of 0.5 nM. In a panel of 384 kinases, only five kinases were inhibited by BMS-986142 with less than 100-fold selectivity for BTK (TEC, ITK, BLK, TXK and BMX).

Targets

BTK [1]
(Cell-free assay)
0.5 nM

In vitro

In B cells stimulated through the B cell receptor (BCR), BMS-986142 potently inhibits signaling and functional end points, including calcium flux (IC50 = 9 nM), production of cytokines, proliferation, and surface expression of the costimulatory molecule CD86 (IC50 = 3−4 nM). In T cells, ITK-catalyzed phosphorylation of PLCγ1 stimulated through the T cell receptor (TCR) is at least 45-fold less potently inhibited by BMS-986142 than BTK-dependent signaling end points in B cells, as expected based on the 30-fold selectivity for BTK over ITK in the enzymatic assays.