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]. IT-901 (12-20 mg/kg; IP) improves the PK profile by increasing T1/2 and Cmax[1]. Animal Model: BALB/C-Tg (NFkB-RE-luc)-Xen mice with 6-9 weeks old[1] Dosage: 24 mg/kg Administration: IP; every other day for 2 weeks Result: Had an effective treatment of acute GVHD without impairing anti-tumor activity.
In Vitro
IT-901 (1, 3, 5 μM; for 24 hours) results in 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]. 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]. 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]. 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]. Cell Proliferation Assay[1] Cell Line: TMD8 and SU-DHL8 cells Concentration: 1, 3, 5 μM Incubation Time: For 24 hours Result: Resulted in decreased proliferation of viable ABC and GCB DLBCL cells. Cell Viability Assay[1] Cell Line: SU-DHL8 and TMD8 cells Concentration: 3 μM Incubation Time: For 24 hours Result: Decreased cell viability in a dose-dependent fashion. Western Blot Analysis[2] Cell Line: Primary chronic lymphocytic leukemia (CLL) cells and cell lines Concentration: 1, 5, 10 μM Incubation Time: For 6 hours Result: Documented Diminished expression of p65 and p50 in nuclear and cytosolic fractions and also decreased the expression of the inhibitory subunit IκBα both in the phosphorylated and non-phosphorylated forms.
Kinase Assay
Cell Assay
Animal Administration
References
Return Policy
If you are in any way unsatisfied with your purchase, you may return any item(s) within 365 days of its original purchase date.
Please provide your Order Number in the email. We strive to reply to all email inquiries within one business day.
