Name | PyriMido[5',4':5,6]pyriMido[1,2-a]benziMidazol-5(6H)-one, 6-(2,6-diMethylphenyl)-2-[[4-(4-Methyl-1-piperazinyl)phenyl]aMino]- |
Synonyms | Lck Inhibitor |
CAS | 847950-09-8 |
Molecular Formula | C31H30N8O |
Molar Mass | 530.62 |
Density | 1.36±0.1 g/cm3(Predicted) |
Boling Point | 809.1±75.0 °C(Predicted) |
pKa | 7.87±0.42(Predicted) |
Storage Condition | 2-8℃ |
In vitro study | Lck Inhibitor (compound 25) exhibits good potency in the T-cell receptor-induced IL-2 secretion assay (IL-2, IC 50 =0.46 μM) and also inhibits subsequent T-cell proliferation (T-cell prolif, IC 50 =0.53 μM) in the same human T-cells. Lck Inhibitor also inhibits a human mixed lymphocyte reaction (huMLR) with a 10-fold increase in potency as compared to the other invitro cell assays utilizing purified human cells. Lck Inhibitor also displays inhibition of a mechanism-based biochemical cell assay probing Lck-dependent TCR-chain phosphorylation (TCR-chain). Lck Inhibitor shows a 10-fold reduction in potency when IL-2 is induced in a receptor-independent fashion by stimulating with phorbo lester and calcium ionophore (PMA/iono). Lck Inhibitor exhibits a similar level of potency when tested in a general proliferation assay using the human T-cell line, Jurkat (JKT). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.885 ml | 9.423 ml | 18.846 ml |
5 mM | 0.377 ml | 1.885 ml | 3.769 ml |
10 mM | 0.188 ml | 0.942 ml | 1.885 ml |
5 mM | 0.038 ml | 0.188 ml | 0.377 ml |