IT-901 NEW
| Price | $122 | $197 | $413 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-06 |
Product Details
| Product Name: IT-901 | CAS No.: 1584121-99-2 |
| Purity: 98.06% | Supply Ability: 10g |
| Release date: 2024/11/06 |
Product Introduction
Bioactivity
| 名稱 | IT-901 |
| 描述 | IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with IC50 values 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. |
| 體外活性 | 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]. |
| 體內(nèi)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]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 10 mg/mL (29.21 mM), Sonication is recommended. |
| 關(guān)鍵字 | IT901 | IT-901 | IT 901 |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 抑制劑庫 | 已知活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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