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。
| 生物活性 | IT-901 is an orally active and potentNF-κBsubunitc-Relinhibitor with anIC50of 0.1 μM, 3 μM forNF-κBDNA binding andc-RelDNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD)[1][2]. |
IC50& Target[1]c-Rel 3 μM (IC50) | NF-κB 0.1 μM (IC50) |
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体外研究
(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 IC50of 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 IC50values 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. |
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体内研究
(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[1].
IT-901 (12-20 mg/kg; IP) improves the PK profile by increasing T1/2and 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 12.5 mg/mL(36.51 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.9208 mL | 14.6041 mL | 29.2082 mL | | 5 mM | 0.5842 mL | 2.9208 mL | 5.8416 mL | | 10 mM | 0.2921 mL | 1.4604 mL | 2.9208 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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