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BMS-986142 potently inhibits human recombinant BTK with an IC50 of 0.5 nM in enzymatic assays. 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. When Ramos B cells are treated with anti-IgM to activate BCR, BMS-986142 inhibits BTK-dependent calcium flux with an IC50 of 9 nM.
In vivo, 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.
| Molecular Weight | 572.60 |
| Formula | C32H30F2N4O4 |
| CAS Number | 1643368-58-4 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related BTK Products |
|---|
| PCI-32765
PCI-32765 (Ibrutinib) is a potent, selective and orally bioavailable irreversible inhibitor of BTK with IC50 value of 0.46 nM. |
| Spebrutinib (AVL-292)
Spebrutinib (AVL-292) is an oral, potent and selective small molecule covalent inhibitor of Btk (IC50 < 0.5 nM). |
| CNX-774
CNX-774 is an irreversible, orally active, and highly selective BTK inhibitor with IC50 of <1 nM. |
| GDC-0834
GDC-0834 is a novel potent and selective BTK inhibitor with IC50 of 5.9 nM. |
| CGI1746
CGI1746 is a potent and highly selective small-molecule inhibitor of the Btk with IC50 of 1.9 nM. |
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Products are for research use only. Not for human use. We do not sell to patients.
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