IT-901 is an orally active and effective inhibitor of NF-Κb subunit c-Rel (IC50s: 0.1 μM, 3 μM for NF-Κb DNA binding and c-Rel DNA binding, respectively). IT-901 has the potential for human lymphoid tumors, and ameliorate gRaft-versus-host disease.

IT-901 is an orally active and effective inhibitor of NF-κB subunit c-Rel (IC50s: 0.1 μM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively). IT-901 has the potential for human lymphoid tumors, and ameliorate graft-versus-host disease.

The concentrations of IT-901 above 10 μM become increasingly toxic and may lead to apoptosis of healthy cells[1]. IT-901 inhibits cell growth of both activated B-like (ABC) and germinal center B-like (GCB) cell lines with the IC50 values between 3μM to 4μM[1]. IT-901 (1, 3, 5 μM; for 24 hours) causes decreased proliferation of viable ABC and GCB DLBCL cells[1]. IT-901 (3 μM; for 24 hours) decreases cell viability in a dose-dependent fashion, at least 60 percent of cells were still viable after 48 hours of IT-901 treatment (4μM) in all tested cell lines except HBL1[1]. The IC50 of IT-901/GDM-12 is 2.9 μM for c-Rel whereas IL-2 secretion is successfully blocked at 5 μM[1]. IT-901 (1, 5, 10 μM; for 6 hours) documents Diminished expression of p65 and p50 in nuclear and cytosolic fractions and also decreases the expression of the inhibitory subunit IκBα both in the phosphorylated and non-phosphorylated forms in primary CLL cells and cell lines[2].

IT-901 (12-20 mg/kg; IP) improves the PK profile by increasing T1/2 and Cmax. IT-901 (24 mg/kg; IP; every other day for 2 weeks) has an effective treatment of acute GVHD without impairing anti-tumor activity[1].

1584121-99-2

C17H14N2O4S

342.37

IT-901

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years