QL47 is a potent, selective and irreversible BTK kinase inhibitor with IC50 of 7 nM.IC50 Value: 7 nMTarget: Btkin vitro: QL47 inhibits BTK kinase activity with an IC50 of 7 nM, inhibits autophosphorylation of BTK on Tyr223 in cells with an EC50 of 475 nM and inhibits phosphorylation of a downstream effector PLCγ2 (Tyr759) with an EC50 of 318 nM. In Ramos cells QL47 induces a G1 cell cycle arrest which is associated with pronounced degradation of BTK protein. QL47 inhibits the proliferation of B-cell lymphoma cancer cell lines at submicromolar concentrations [1].in vivo: N/A
[1]. Wu, H., et al., Discovery of a Potent, Covalent BTK Inhibitor for B-Cell Lymphoma. ACS Chem Biol, 2014.