Powder: -20°C for 3 years | In solvent: -80°C for 1 year
IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 for NF-κB and c-Rel binding to DNA of 0.1 µM and 3 µM, respectively.IT-901 is a naphthalene thiobarbiturate derivative with antitumor activity and is used for the prevention and treatment of human lymphoma and myeloma.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 122.00 | |
10 mg | In stock | $ 197.00 | |
25 mg | In stock | $ 413.00 | |
50 mg | In stock | $ 663.00 | |
100 mg | In stock | $ 1,060.00 |
Description | IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 for NF-κB and c-Rel binding to DNA of 0.1 µM and 3 µM, respectively.IT-901 is a naphthalene thiobarbiturate derivative with antitumor activity and is used for the prevention and treatment of human lymphoma and myeloma. |
Targets&IC50 | NF-κB:0.1 μM, c-Rel:2.9μM, GCB:4 μ M |
In vitro |
Following 24 hours of treatment with IT-901 at concentrations of 1, 3, and 5 μM, there is a reduction in the proliferation of viable ABC and GCB DLBCL cells[2]. At a concentration of 3 μM and a duration of 24 hours, IT-901 induces a dose-dependent decrease in cell viability. However, at least 60 percent of cells remain viable after 48 hours of treatment with 4 μM IT-901 in all tested cell lines, except HBL1[2]. With a treatment duration of 6 hours and concentrations of 1, 5, and 10 μM, IT-901 leads to a diminished expression of p65 and p50 in both nuclear and cytosolic fractions. Additionally, it reduces the expression of the inhibitory subunit IκBα in both 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, while IL-2 secretion is effectively blocked at 5 μM[2]. Concentrations of IT-901 above 10 μM become increasingly toxic and may induce apoptosis in healthy cells[2]. IT-901 demonstrates inhibition of cell growth in both activated B-like (ABC) and germinal center B-like (GCB) cell lines, with IC50 values ranging between 3 μM to 4 μM[2]. |
In vivo |
Administered intraperitoneally (IP) every other day for 2 weeks at a dose of 24 mg/kg, IT-901 proves to be an effective treatment for acute graft-versus-host disease (GVHD) without compromising its anti-tumor activity[2]. IT-901, given at doses ranging from 12 to 20 mg/kg via IP administration, enhances the pharmacokinetic (PK) profile by increasing both half-life (T1/2) and maximum plasma concentration (Cmax)[2]. |
Molecular Weight | 342.37 |
Formula | C17H14N2O4S |
CAS No. | 1584121-99-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mg/mL (29.21 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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IT-901 1584121-99-2 Others IT901 IT 901 inhibitor inhibit