Cas No.: | 1469988-75-7 |
Chemical Name: | Benzo[h]-1,6-naphthyridin-2(1H)-one, 1-[2,3-dihydro-1-(1-oxo-2-propen-1-yl)-1H-indol-6-yl]-9-(1-methyl-1H-pyrazol-4-yl)- |
SMILES: | O=C1C=CC2C=NC3C(C=2N1C1C=C2N(C(=O)C=C)CCC2=CC=1)=CC(C1C=NN(C)C=1)=CC=3 |
Formula: | C27H21N5O2 |
M.Wt: | 447.4879 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | A potent, selective, and irreversible BTK inhibitor with IC50 of 7 nM; 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; induces a G1 cell cycle arrest that is associated with pronounced degradation of BTK protein in Ramos cells; inhibits the proliferation of B-cell lymphoma cancer cell lines at submicromolar concentrations. Blood CancerPreclinical |