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IT-901

产品编号 T15601 CAS 1584121-99-2

IT-901 是一种具有口服活性和有效性的 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 和 3 μM。IT-901 是一种具有抗肿瘤活性的萘硫代巴比妥酸酯衍生物，可用于预防和治疗人类淋巴瘤和骨髓瘤。

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IT-901, CAS 1584121-99-2

规格	价格/CNY	货期
1 mg	￥ 1,290	现货
2 mg	￥ 1,830	现货
5 mg	￥ 2,880	现货
10 mg	￥ 4,630	现货
25 mg	￥ 7,150	现货
50 mg	￥ 9,630	现货
100 mg	￥ 12,900	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	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.
靶点活性	NF-κB:0.1 μM, c-Rel:2.9μM, GCB:4 μ M
体外活性	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].
体内活性	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].

分子量	342.37
分子式	C17H14N2O4S
CAS No.	1584121-99-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 10 mg/mL (29.21 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9208 mL	14.6041 mL	29.2082 mL	73.0204 mL
	5 mM	0.5842 mL	2.9208 mL	5.8416 mL	14.6041 mL
	10 mM	0.2921 mL	1.4604 mL	2.9208 mL	7.302 mL
	20 mM	0.146 mL	0.7302 mL	1.4604 mL	3.651 mL

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参考文献

1. Vaisitti T, et al. Targeting metabolism and survival in chronic lymphocytic leukemia and Richter syndrome cellsby a novel NF-κB inhibitor. Haematologica. 2017 Nov;102(11):1878-1889. 2. Shono Y, et al. Characterization of a c-Rel Inhibitor That Mediates Anticancer Properties in HematologicMalignancies by Blocking NF-κB-Controlled Oxidative Stress Responses. Cancer Res. 2016 Jan 15;76(2):377-89.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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