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IT-901

CAS No. : 1584121-99-2

MCE 站：IT-901

产品活性：IT-901 是一种具有口服活性且有效的 NF-κB 亚基 c-Rel 抑制剂，对 NF-κB 和 c-Rel 与 DNA 结合的 IC₅₀ 分别为 0.1 µM，3 μM。IT-901 是一种具有生物活性的萘硫代巴比妥酸酯衍生物，具有用于人类淋巴瘤和改善移植物抗宿主病 (GVHD) 的潜力。

研究领域：NF-κB

作用靶点：NF-κB

In Vitro: IT-901 (1, 3, 5 μM; for 24 hours) results in decreased proliferation of viable ABC ａnd GCB DLBCL cells.
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.
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.
The IC₅₀ of IT-901/GDM-12 is 2.9 μM for c-Rel whereas IL-2 secretion is successfully blocked at 5 μM.
The concentrations of IT-901 above 10 μM become increasingly toxic ａnd may lead to apoptosis of healthy cells.
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.

In Vivo: IT-901 (24 mg/kg; IP; every other day for 2 weeks) has an effective treatment of acute GVHD without impairing anti-tumor activity.
IT-901 (12-20 mg/kg; IP) improves the PK profile by increasing T_1/2 ａnd C_max.

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